Erlotinib
别名: CP358774, NSC 718781,OSI-774 中文名称：厄洛替尼,埃罗替尼
Erlotinib是一种EGFR抑制剂，IC50 为 2 nM，对EGFR的敏感性比对人c-Src 或 v-Ab高1000多倍。Erlotinib可诱导自噬。
Erlotinib Chemical Structure
CAS: 183321-74-6
产品质控
批次：
纯度：
99.99%
99.99
Erlotinib相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| LLC | Antitumor assay | 100 mg/kg | 14 days | Antitumor activity against mouse LLC cells allografted in SCID mouse assessed as inhibition of tumor growth at 100 mg/kg, po qd for 14 days | 26188620 |
| PC9 | Antitumor assay | 15 mg/kg | 4 weeks | Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse assessed as tumor regression at 15 mg/kg, qd measured after 4 weeks | 26313252 |
| PC9 | Antitumor assay | 15 mg/kg | 4 weeks | Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse at 15 mg/kg, qd measured after 4 weeks | 26313252 |
| hematopoietic progenitor cells | Growth inhibition assay | 5 uM | Growth inhibition of JAK2 V617F mutant expressing human polycythemia vera hematopoietic progenitor cells at 5 uM by erythroid burst-forming unit assay | 17178722 | |
| PC9 | Cytotoxicity assay | 0.001 to 10 uM | Cytotoxicity against human PC9 cells expressing 746-750 sequence deleted EGFR assessed as cell viability at 0.001 to 10 uM after 96 hrs by cell titer-glo assay | 20222733 | |
| NCI-H1975 | Cytotoxicity assay | 0.001 to 10 uM | Cytotoxicity against human NCI-H1975 cells expressing EGFR T790M and L858R mutant at 0.001 to 10 uM after 96 hrs by cell titer-glo assay | 20222733 | |
| HCC827 | Apoptosis assay | 1 uM | Induction of apoptosis in human HCC827 cells at 1 uM after 24 hrs using propidium iodide by flow cytometry | 24900830 | |
| Huh7.5 | Antiviral assay | 30 mins | Antiviral activity against Hepatitis C virus J6/JFH infected in human Huh7.5 cells assessed as inhibition of HCV replication pretreated for 30 mins followed by infection measured after 72 hrs by alamar blue dye based fluorescence assay | 26925208 | |
| Huh7.5 | Antiviral assay | 72 hrs | Antiviral activity against Hepatitis C virus J6/JFH infected in human Huh7.5 cells assessed as inhibition of viral replication measured after 72 hrs by luciferase reporter gene assay, EC50 = 0.5 μM. | 25822739 | |
| Huh7.5 | Antiviral assay | 72 hrs | Antiviral activity against Hepatitis C virus J6/JFH electroporated in human Huh7.5 cells assessed as inhibition of intracellular infectivity drug treated every 24 hrs for 72 hrs measured 72 hrs post electroporation by luciferase reporter gene assay, EC50 = 0.5 μM. | 25822739 | |
| Huh7.5 | Antiviral assay | 72 hrs | Antiviral activity against Hepatitis C virus J6/JFH infected in human Huh7.5 cells assessed as inhibition of extracellular infectivity drug treated every 24 hrs for 72 hrs measured after 72 hrs by luciferase reporter gene assay, EC50 = 0.5 μM. | 25822739 | |
| NCI-H292 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR after 72 hrs by luminescence assay, EC50 = 0.031 μM. | 26455919 | |
| A431 | Growth inhibition assay | 72 hrs | Growth inhibition of human A431 cells overexpressing EGFR after 72 hrs by MTT assay, GI50 = 0.47 μM. | 17983745 | |
| A431 | Growth inhibition assay | 72 hrs | Growth inhibition of human A431 cells after 72 hrs by MTT assay, GI50 = 0.915 μM. | 19969465 | |
| BA/F3 | Growth inhibition assay | 96 hrs | Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay, GI50 = 0.5 μM. | 20222733 | |
| BA/F3 | Growth inhibition assay | 96 hrs | Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay, GI50 = 0.5 μM. | 20222733 | |
| BA/F3 | Growth inhibition assay | 96 hrs | Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay, GI50 = 0.5 μM. | 20222733 | |
| BA/F3 | Growth inhibition assay | 96 hrs | Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay, GI50 = 0.5 μM. | 20222733 | |
| WM266.4 | Growth inhibition assay | 24 hrs | Growth inhibition in human WM266.4 cells after 24 hrs by MTT reduction assay, GI50 = 8.12 μM. | 22985962 | |
| A549 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human A549 cells after 24 hrs by MTT assay, GI50 = 0.03 μM. | 23391364 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, GI50 = 0.08 μM. | 23391364 | |
| WM266.4 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human WM266.4 cells assessed as cell viability after 24 hrs by MTT assay, GI50 = 8.14 μM. | 27238841 | |
| Jurkat | Growth inhibition assay | 24 hrs | Growth inhibition of human Jurkat cells after 24 hrs, IC50 = 2 μM. | 17178722 | |
| erythroleukemia cells | Growth inhibition assay | 24 hrs | Growth inhibition of JAK2 V617F mutant expressing human erythroleukemia cells after 24 hrs, IC50 = 2 μM. | 17178722 | |
| erythroleukemia cells | Growth inhibition assay | 24 hrs | Growth inhibition of mouse erythroleukemia cells after 24 hrs, IC50 = 2 μM. | 17178722 | |
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50 = 0.096 μM. | 19888761 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. | 19914835 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.01 μM. | 19914837 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. | 20005116 | |
| A431 | Function assay | 10 mins | Inhibition of EGFR phosphorylation in human A431 cells after 10 mins by FLISA, IC50 = 1.2 μM. | 20403700 | |
| NCI-H661 | Cytotoxicity assay | 4 to 5 days | Cytotoxicity against human NCI-H661 cells after 4 to 5 days by MTT assay, IC50 = 12.71 μM. | 20466555 | |
| DU145 | Cytotoxicity assay | 4 to 5 days | Cytotoxicity against human DU145 cells after 4 to 5 days by MTT assay, IC50 = 19.4 μM. | 20466555 | |
| A549 | Cytotoxicity assay | 4 to 5 days | Cytotoxicity against human A549 cells after 4 to 5 days by MTT assay, IC50 = 33.03 μM. | 20466555 | |
| PC3 | Cytotoxicity assay | 4 to 5 days | Cytotoxicity against human PC3 cells after 4 to 5 days by MTT assay, IC50 = 36.76 μM. | 20466555 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. | 20594859 | |
| Sf9 | Function assay | 1 hr | Inhibition of human recombinant His6x-tagged EGFR autophosphorylation expressed in Sf9 cells after 1 hr by ELISA, IC50 = 0.03 μM. | 20594859 | |
| Sf9 | Function assay | 1 hr | Inhibition of human recombinant His6x-tagged HER2 autophosphorylation expressed in Sf9 cells after 1 hr by ELISA, IC50 = 0.16 μM. | 20594859 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. | 20627597 | |
| Sf9 | Function assay | 1 hr | Inhibition of recombinant EGFR expressed in baculovirus infected Sf9 cells after 1 hr by DELFIA/time-resolved fluorimetry assay, IC50 = 0.03 μM. | 21763148 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells expressing EGFR assessed as inhibition of basal cell growth after 48 hrs by MTT assay, IC50 = 0.27 μM. | 21763148 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. | 21802290 | |
| Sf9 | Function assay | 1 hr | Inhibition of His-tagged EGFR expressed in insect Sf9 cells after 1 hr by time-resolved fluorimetric analysis, IC50 = 0.03 μM. | 21816517 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.08 μM. | 21816517 | |
| A16-F10 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A16-F10 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. | 22112541 | |
| Sf9 | Function assay | 10 mins | Inhibition of EGFR expressed in baculovirus infected Sf9 cells assessed as inhibition of autophosphorylation preincubated for 10 mins measured after 1 hr by DELFIA/Time-Resolved Fluorometry, IC50 = 0.03 μM. | 22112541 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. | 22112541 | |
| DIFI | Cytotoxicity assay | 4 days | Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.14 μM. | 22169601 | |
| CAL27 | Cytotoxicity assay | 4 days | Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.239 μM. | 22169601 | |
| GXF251L | Cytotoxicity assay | 4 days | Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.369 μM. | 22169601 | |
| LXFA 629L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 629L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.66 μM. | 22169601 | |
| DU145 | Cytotoxicity assay | 4 days | Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.966 μM. | 22169601 | |
| LXFA 289L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 289L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 1.78 μM. | 22169601 | |
| LNCAP | Cytotoxicity assay | 4 days | Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.63 μM. | 22169601 | |
| OVXF 899L | Cytotoxicity assay | 4 days | Cytotoxicity against human OVXF 899L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.77 μM. | 22169601 | |
| PAXF 546L | Cytotoxicity assay | 4 days | Cytotoxicity against human PAXF 546L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10 μM. | 22169601 | |
| RXF 486L | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 486L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10 μM. | 22169601 | |
| BXF T24 | Cytotoxicity assay | 4 days | Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.9 μM. | 22169601 | |
| CXF 269L | Cytotoxicity assay | 4 days | Cytotoxicity against human CXF 269L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 16 μM. | 22169601 | |
| PC3M | Cytotoxicity assay | 4 days | Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 17.2 μM. | 22169601 | |
| LXFL 529L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFL 529L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 17.4 μM. | 22169601 | |
| MEXF 276L | Cytotoxicity assay | 4 days | Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 18.6 μM. | 22169601 | |
| Saos2 | Cytotoxicity assay | 4 days | Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 21 μM. | 22169601 | |
| UXF 1138L | Cytotoxicity assay | 4 days | Cytotoxicity against human UXF 1138L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 24.5 μM. | 22169601 | |
| MAXF 401NL | Cytotoxicity assay | 4 days | Cytotoxicity against human MAXF 401NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 25 μM. | 22169601 | |
| MEXF 1341L | Cytotoxicity assay | 4 days | Cytotoxicity against human MEXF 1341L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 30.1 μM. | 22169601 | |
| PXF 1752L | Cytotoxicity assay | 4 days | Cytotoxicity against human PXF 1752L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 31.6 μM. | 22169601 | |
| MDA231 | Cytotoxicity assay | 4 days | Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 34.5 μM. | 22169601 | |
| LXFL 1121L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFL 1121L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 34.6 μM. | 22169601 | |
| PXF 698L | Cytotoxicity assay | 4 days | Cytotoxicity against human PXF 698L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 36.4 μM. | 22169601 | |
| RXF 393NL | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 45.6 μM. | 22169601 | |
| LIXF 575L | Cytotoxicity assay | 4 days | Cytotoxicity against human LIXF 575L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 47.2 μM. | 22169601 | |
| A431 | Function assay | 60 mins | Inhibition of EGFR tyrosine kinase activity in EGF-stimulated human A431 cells after 60 mins by ELISA, IC50 = 1.2 μM. | 22204741 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. | 22277588 | |
| Sf9 | Function assay | 1 hr | Inhibition of autophosphorylation of recombinant His-tagged EGFR expressed in baculovirus infected Sf9 cells after 1 hr by DELFIA/time-resolved fluorimetry assay, IC50 = 0.03 μM. | 22277588 | |
| Sf9 | Function assay | 1 hr | Inhibition of histidine-tagged human recombinant cytoplasmic domain of EGFR expressed in baculovirus infected insect Sf9 cells after 1 hr by DELFIA/time-resolved fluorometric analysis, IC50 = 0.03 μM. | 22361272 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.07 μM. | 22361272 | |
| B16F10 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. | 22361272 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 0.14 μM. | 22361272 | |
| Sf9 | Function assay | 1 hr | Inhibition of histidine-tagged human recombinant cytoplasmic domain of HER2 expressed in baculovirus infected insect Sf9 cells after 1 hr by DELFIA/time-resolved fluorometric analysis, IC50 = 0.14 μM. | 22361272 | |
| A431 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A431 cells over expressing EGFR after 48 hrs by MTT assay, IC50 = 0.055 μM. | 22414612 | |
| HEK293 Flp-In | Function assay | 5 mins | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, IC50 = 0.55 μM. | 22541068 | |
| HEK293 Flp-In | Function assay | 5 mins | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, IC50 = 44 μM. | 22541068 | |
| A431 | Function assay | 60 mins | Inhibition of EGFR in human A431 cells pretreated for 60 mins measured after 1 hr by ELISA, IC50 = 1.2 μM. | 22739090 | |
| SF539 | Function assay | 60 mins | Inhibition of PDGFRbeta in human SF539 cells pretreated for 60 mins measured after 1 hr by ELISA, IC50 = 12.2 μM. | 22739090 | |
| PC9 | Function assay | 24 hrs | Inhibition of EGFR phosphorylation in human PC9 cells after 24 hrs by by Western blot analysis, IC50 = 1.36 μM. | 22980218 | |
| WM266.4 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human WM266.4 cells after 24 hrs by MTT assay, IC50 = 8.09 μM. | 22985957 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 8.97 μM. | 22985957 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. | 23245570 | |
| A16-F10 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A16-F10 cells after 48 hrs by MTT assay, IC50 = 0.2 μM. | 23245570 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. | 23245802 | |
| B16/F10 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse B16/F10 cells after 48 hrs by MTT assay, IC50 = 0.05 μM. | 23245802 | |
| A431 | Function assay | 60 mins | Inhibition of EGF-induced EGFR phosphorylation in human A431 cells overexpressing EGFR pretreated for 60 mins prior to EGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis, IC50 = 1.2 μM. | 23375090 | |
| SF539 | Function assay | 60 mins | Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis, IC50 = 12.2 μM. | 23375090 | |
| A431 | Function assay | 60 mins | Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA, IC50 = 1.2 μM. | 23434139 | |
| SF539 | Function assay | 60 mins | Inhibition of PDGFRbeta in human SF539 cells assessed as inhibition of PDGFR-BB-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA, IC50 = 12.2 μM. | 23434139 | |
| PC9 | Function assay | 2 hrs | Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay, IC50 = 0.0059 μM. | 23930994 | |
| LoVo | Function assay | 2 hrs | Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay, IC50 = 0.077 μM. | 23930994 | |
| NCI-H1975 | Function assay | 2 hrs | Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay, IC50 = 7.6 μM. | 23930994 | |
| Sf9 | Function assay | 10 mins | Inhibition of recombinant EGFR kinase cytoplasmic domain (unknown origin) expressed in baculovirus expression vector-infected insect sf9 cells assessed as level of autophosphorylation after 10 mins by DELFIA/time-resolved fluorometry, IC50 = 0.03 μM. | 23962660 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. | 23962660 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.13 μM. | 23962660 | |
| Sf9 | Function assay | 10 mins | Inhibition of recombinant EGFR cytoplasmic domain (645 to 1186) (unknown origin) autophosphorylation expressed in baculovirus infected insect Sf9 cells preincubated for 10 mins followed by ATP-MgCl2 addition measured after 1 hr by fluorometric analysis, IC50 = 0.032 μM. | 24144854 | |
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.12 μM. | 24144854 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.13 μM. | 24144854 | |
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells after 72 hrs by SRB assay, IC50 = 0.409 μM. | 24183742 | |
| NCI-H1975 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M mutant after 72 hrs by SRB assay, IC50 = 6.9 μM. | 24183742 | |
| KB | Function assay | 1 hr | Inhibition of EGF-stimulated autophosphorylation of EGFR in human KB cells incubated for 1 hr prior to EGF challenge measured after 6 mins by ELISA, IC50 = 0.019 μM. | 24411123 | |
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells expressing EGFR after 72 hrs by MTT assay, IC50 = 0.75 μM. | 24411123 | |
| Calu3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Calu3 cells expressing HER2 after 72 hrs by MTT assay, IC50 = 0.93 μM. | 24411123 | |
| NCI-H1975 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50 = 5.51 μM. | 24411123 | |
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 0.56 μM. | 24565969 | |
| NCI-H1975 | Antiproliferative assay | 72 hrs | Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 7.06 μM. | 24565969 | |
| Sf9 | Function assay | 1 hr | Inhibition of autophosphorylation of recombinant EGFR cytoplasmic domain (645 to 1186) (unknown origin) expressed in Sf9 cells after 1 hr by DELFIA/time-resolved fluorometric analysis, IC50 = 0.032 μM. | 24607998 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. | 24607998 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.13 μM. | 24607998 | |
| Sf9 | Function assay | 1 hr | Inhibition of autophosphorylation of EGFR cytoplasmic domain (amino acids 645 to 1186) (unknown origin) expressed in Sf9 cells after 1 hr by time-resolved fluorometry, IC50 = 0.032 μM. | 24630412 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. | 24630412 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.13 μM. | 24630412 | |
| Sf9 | Function assay | 1 hr | Inhibition of autophosphorylation of human HER2 cytoplasmic domain (amino acids 676 to 1245) (unknown origin) expressed in Sf9 cells after 1 hr by time-resolved fluorometry, IC50 = 0.16 μM. | 24630412 | |
| HCC827 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay, IC50 = 0.002 μM. | 24900830 | |
| NCI-H1993 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay, IC50 = 2.043 μM. | 24900830 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 7.099 μM. | 24900830 | |
| NCI-H1975 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay, IC50 = 7.498 μM. | 24900830 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. | 25172421 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. | 25172421 | |
| NCI-H292 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-H292 cells after 72 hrs by SRB assay, IC50 = 1 μM. | 25215856 | |
| H460 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human H460 cells after 72 hrs by SRB assay, IC50 = 9.5 μM. | 25215856 | |
| H460/Vbl | Cytotoxicity assay | 72 hrs | Cytotoxicity against human H460/Vbl cells after 72 hrs by SRB assay, IC50 = 21.5 μM. | 25215856 | |
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation under normoxia conditions after 72 hrs by SRB assay, IC50 = 2.98 μM. | 25468044 | |
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation under hypoxia conditions after 72 hrs by SRB assay, IC50 = 4.37 μM. | 25468044 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation under normoxia conditions after 72 hrs by SRB assay, IC50 = 7.59 μM. | 25468044 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation under hypoxia conditions after 72 hrs by SRB assay, IC50 = 9.1 μM. | 25468044 | |
| A431 | Function assay | 60 min | Inhibition of EGFR in human A431 cells compound pretreated for 60 min before EGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.0012 μM. | 25882519 | |
| U251 | Function assay | 60 min | Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.1247 μM. | 25882519 | |
| KB | Antiproliferative assay | 48 hrs | Antiproliferative activity against human KB cells expressing EGFR and Src after 48 hrs by SRB assay, IC50 = 5 μM. | 26188620 | |
| A498 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A498 cells expressing EGFR and Src after 48 hrs by SRB assay, IC50 = 25.6 μM. | 26188620 | |
| NCI-H292 | Function assay | 1 hr | Inhibition of EGFR phosphorylation in human NCI-H292 cells preincubated for 1 hr followed by stimulation with EGF for 8 mins by electrochemiluminescent immunoassay, IC50 = 0.0063 μM. | 26455919 | |
| HCC827 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCC827 cells after 72 hrs by CCK-8 assay, IC50 = 0.029 μM. | 26487917 | |
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells after 72 hrs by CCK-8 assay, IC50 = 0.844 μM. | 26487917 | |
| PANC1 | Growth inhibition assay | 72 hrs | Growth inhibition of human PANC1 cells after 72 hrs by CCK-8 assay, IC50 = 3.1 μM. | 26547690 | |
| L3.6PL | Growth inhibition assay | 72 hrs | Growth inhibition of human L3.6PL cells after 72 hrs by CCK-8 assay, IC50 = 4 μM. | 26547690 | |
| PCI35 | Growth inhibition assay | 72 hrs | Growth inhibition of human PCI35 cells after 72 hrs by CCK-8 assay, IC50 = 7.7 μM. | 26547690 | |
| PC9 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human PC9 cells after 96 hrs by Sytox green marker based fluorescence analysis, IC50 = 0.07 μM. | 26599532 | |
| H9 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human H9 cells after 72 hrs by CellTiter-Glo assay, IC50 = 1.3 μM. | 26599532 | |
| OVCAR3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human OVCAR3 cells after 72 hrs by CellTiter-Glo assay, IC50 = 4.6 μM. | 26599532 | |
| Calu3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Calu3 cells after 72 hrs by CellTiter blue assay, IC50 = 4.7 μM. | 26599532 | |
| MRC5 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MRC5 cells after 72 hrs by CellTiter-Glo assay, IC50 = 5.8 μM. | 26599532 | |
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells after 72 hrs by CellTiter blue assay, IC50 = 9.9 μM. | 26599532 | |
| BT474 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human BT474 cells after 72 hrs by CellTiter blue assay, IC50 = 13 μM. | 26599532 | |
| MCF7 | Antiproliferative assay | 12 hrs | Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay, IC50 = 0.1 μM. | 26652482 | |
| HepG2 | Antiproliferative assay | 12 hrs | Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay, IC50 = 0.12 μM. | 26652482 | |
| B16F10 | Antiproliferative assay | 12 hrs | Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay, IC50 = 0.17 μM. | 26652482 | |
| HeLa | Antiproliferative assay | 12 hrs | Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay, IC50 = 0.2 μM. | 26652482 | |
| HCC827 | Function assay | 2 hrs | Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISA, IC50 = 0.008 μM. | 26756222 | |
| H3255 | Function assay | 2 hrs | Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISA, IC50 = 0.01 μM. | 26756222 | |
| PC9 | Function assay | 2 hrs | Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA, IC50 = 0.011 μM. | 26756222 | |
| NCI-H1975 | Function assay | 2 hrs | Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA, IC50 = 9 μM. | 26756222 | |
| PC9-DRH | Function assay | 2 hrs | Inhibition of EGFR deletion/T790M mutant autophosphorylation in human PC9-DRH cells after 2 hrs by sandwich ELISA, IC50 = 9.7 μM. | 26756222 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells assessed as viable cells after 48 hrs by CCK8 assay, IC50 = 6.26 μM. | 26879314 | |
| NCI-H358 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human NCI-H358 cells assessed as viable cells after 48 hrs by CCK8 assay, IC50 = 6.85 μM. | 26879314 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 5.8 μM. | 26896708 | |
| LO2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human LO2 cells after 48 hrs by MTT assay, IC50 = 18.5 μM. | 26896708 | |
| NCI-H358 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 48 hrs by cck8 assay, IC50 = 3.91 μM. | 27234887 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by cck8 assay, IC50 = 7.35 μM. | 27234887 | |
| BA/F3 | Function assay | 48 hrs | Inhibition of EGFR L858R mutant (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by XTT assay, IC50 = 0.087 μM. | 27235841 | |
| A431 | Function assay | 60 mins | Inhibition of EGFR in human A431 cells assessed as reduction in EGF induced phosphorylation preincubated for 60 mins followed by EGF addition measured after 10 mins by ELISA method, IC50 = 0.0012 μM. | 27894589 | |
| HEK293 | Function assay | 2 mins | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay, IC50 = 16.2 μM. | 28230985 | |
| H3255 | Function assay | 2 hrs | Inhibition of EGFR L858R mutant phosphorylation in human H3255 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 0.01 μM. | 28287730 | |
| A549 | Function assay | 2 hrs | Inhibition of EGF-stimulated wild-type EGFR phosphorylation in human A549 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 0.011 μM. | 28287730 | |
| PC9 | Function assay | 2 hrs | Inhibition of EGFR exon 19 deletion mutant phosphorylation in human PC9 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 0.011 μM. | 28287730 | |
| H1975 | Function assay | 2 hrs | Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 9.003 μM. | 28287730 | |
| PC9-DRH | Function assay | 2 hrs | Inhibition of EGFR T790M/exon 19 deletion mutant phosphorylation in human PC9-DRH cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 9.736 μM. | 28287730 | |
| Sf9 | Function assay | 10 mins | Inhibition of His6-tagged recombinant EGFR cytoplasmic domain (unknown origin) (645 to 1186 residues) expressed in baculovirus infected Sf-9 cells preincubated for 10 mins followed by ATP addition measured after 1 hr by DELFIA/Time-Resolved fluorometry, IC50 = 0.06 μM. | 28431353 | |
| HepG2 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 24 hrs by spectrophotometry, IC50 = 25 μM. | 28487127 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 21.3 μM. | 28886509 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay, IC50 = 30.12 μM. | 28923383 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay, IC50 = 33.46 μM. | 28923383 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.08 μM. | 28988624 | |
| B16F10 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. | 28988624 | |
| A549 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human A549 cells after 24 hrs by MTT assay, IC50 = 0.73 μM. | 29028534 | |
| A498 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 12.5 μM. | 29057042 | |
| HuH7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 25 μM. | 29057042 | |
| NCI-H23 | Cytotoxicity assay | 46 hrs | Cytotoxicity against human NCI-H23 cells assessed as reduction in cell viability after 46 hrs by MTT assay, IC50 = 49.3 μM. | 29138027 | |
| HT-29 | Antiproliferative assay | 48 hrs | Antiproliferative activity human HT-29 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.02 μM. | 29407956 | |
| MIAPaCa2 | Antiproliferative assay | 48 hrs | Antiproliferative activity human MIAPaCa2 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.03 μM. | 29407956 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity human MCF7 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.03 μM. | 29407956 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity human PC3 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.03 μM. | 29407956 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity human A549 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.04 μM. | 29407956 | |
| Sf9 | Function assay | 10 mins | Inhibition of His6-tagged EGFR (unknown origin) cytoplasmic domain expressed in baculovirus infected Sf9 insect cells after 10 mins followed by addition of ATP-MgCl2 and measured after 1 hr by time-resolved fluorometric analysis, IC50 = 0.08 μM. | 29407956 | |
| A549 | Anticancer assay | 96 hrs | Anticancer activity against human A549 cells assessed as reduction in cell viability after 96 hrs by MTT assay, IC50 = 17.32 μM. | 29549841 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 20 μM. | 30047410 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 25 μM. | 30047410 | |
| Sf9 | Function assay | 5 mins | Inhibition of recombinant human GST-tagged HER2 (676-end) expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.091 μM. | 30096580 | |
| Sf9 | Function assay | 5 mins | Inhibition of GST-tagged recombinant human VEGFR (789-end) expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.25 μM. | 30096580 | |
| A431 | Function assay | 60 mins | Inhibition of EGF-induced EGFR activation in human A431 cells pretreated for 60 mins followed by EGF addition and measured after 10 mins by ELISA, IC50 = 0.0012 μM. | 30098869 | |
| U251 | Function assay | 60 mins | Inhibition of VEGF-induced VEGFR2 activation in human U251 cells pretreated for 60 mins followed by VEGF addition and measured after 10 mins by ELISA, IC50 = 0.1247 μM. | 30098869 | |
| HEK293 Flp-In | Function assay | 5 mins | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, Ki = 0.53 μM. | 22541068 | |
| HEK293 Flp-In | Function assay | 5 mins | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, Ki = 41 μM. | 22541068 | |
| A431 | Function assay | 1 hrs | Inhibition of EGF-induced EGFR phosphorylation in human A431 cells pretreated for 1 hrs followed by EGF-stimulation by immunoblot analysis | 19969465 | |
| human A431 cells | Function assay | Inhibition of EGFR in human A431 cells by HTRF assay, IC50=0.42 μM. | 19815412 | ||
| human SKBR3 cells | Function assay | Inhibition of HER2 in human SKBR3 cells by HTRF assay, IC50=1.89 μM. | 19815412 | ||
| NIH3T3 | Function assay | Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells, IC50 = 0.0193 μM. | 16480284 | ||
| T24 NIH | Function assay | Inhibition of ligand stimulated erbB2 autophosphorylation in T24 NIH cells, IC50 = 0.299 μM. | 16480284 | ||
| COS7 | Function assay | Inhibition of human JAK2 V617F mutant expressed in COS7 cells, IC50 = 4 μM. | 17178722 | ||
| hematopoietic progenitor cells | Growth inhibition assay | Growth inhibition of JAK2 V617F mutant expressing hematopoietic progenitor cells isolated from polycythemia vera patient by colony forming assay, IC50 = 5 μM. | 17178722 | ||
| BA/F3 | Cytotoxicity assay | Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R mutant, IC50 = 0.0125 μM. | 19239229 | ||
| Sf9 | Function assay | Inhibition of cloned EGFR autophosphorylation expressed in baculovirus-infected Sf9 cells by solid-phase ELISA, IC50 = 0.03 μM. | 19914835 | ||
| Sf9 | Function assay | Inhibition of human cloned HER2 autophosphorylation expressed in baculovirus-infected Sf9 cells by solid-phase ELISA, IC50 = 0.16 μM. | 19914835 | ||
| Sf9 | Function assay | Inhibition of cloned EGFR autophosphorylation expressed in baculovirus-infected Sf9 cells by solid-phase ELISA, IC50 = 0.02 μM. | 19914837 | ||
| Sf9 | Function assay | Inhibition of human cloned HER2 autophosphorylation expressed in baculovirus-infected Sf9 cells by solid-phase ELISA, IC50 = 0.12 μM. | 19914837 | ||
| NCI-H2122 | Antiproliferative assay | Antiproliferative activity against human NCI-H2122 cells, IC50 = 1 μM. | 20143778 | ||
| SK-BR-3 | Antiproliferative assay | Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay, IC50 = 1.56 μM. | 20143778 | ||
| SCC15 | Antiproliferative assay | Antiproliferative activity against human SCC15 cells, IC50 = 1.94 μM. | 20143778 | ||
| SCC25 | Antiproliferative assay | Antiproliferative activity against human SCC25 cells, IC50 = 3.34 μM. | 20143778 | ||
| NCI-H358 | Antiproliferative assay | Antiproliferative activity against human NCI-H358 cells after hrs by ATP content assay, IC50 = 6 μM. | 20143778 | ||
| HCC827 | Antiproliferative assay | Antiproliferative activity against human HCC827 cells after hrs by ATP content assay, IC50 = 7.5 μM. | 20143778 | ||
| BxPC3 | Antiproliferative assay | Antiproliferative activity against human BxPC3 cells after hrs by ATP content assay, IC50 = 7.6 μM. | 20143778 | ||
| H460 | Antiproliferative assay | Antiproliferative activity against human H460 cells after hrs by ATP content assay, IC50 = 8.2 μM. | 20143778 | ||
| CAL27 | Antiproliferative assay | Antiproliferative activity against human CAL27 cells, IC50 = 10.15 μM. | 20143778 | ||
| SKHEP1 | Antiproliferative assay | Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay, IC50 = 10.37 μM. | 20143778 | ||
| MDA-MB-468 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-468 cells, IC50 = 11.4 μM. | 20143778 | ||
| LNCAP | Antiproliferative assay | Antiproliferative activity against human LNCAP cells, IC50 = 18.35 μM. | 20143778 | ||
| A431 | Function assay | Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.034 μM. | 20346655 | ||
| N87 | Function assay | Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA, IC50 = 5.2 μM. | 20346655 | ||
| A431 | Function assay | Inhibition of EGFR expressed in human A431 cells, IC50 = 1.2 μM. | 20558072 | ||
| Sf9 | Function assay | Inhibition of histidine-tagged recombinant EGFR autophosphorylation expressed in Sf9 cells by solid-phase ELISA, IC50 = 0.03 μM. | 20627597 | ||
| MIAPaCa | Function assay | Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.051 μM. | 20817523 | ||
| MIAPaCa | Function assay | Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISA, IC50 = 6.73 μM. | 20817523 | ||
| HEK293 Flp-In | Function assay | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, IC50 = 21 μM. | 22541068 | ||
| Sf9 | Function assay | Inhibition of EGFR cytoplasmic domain (amino acids 645 to 1186) (unknown origin) expressed in Sf9 cells assessed as reduction in enzyme autophosphorylation by DELFIA time resolved fluorometry, IC50 = 0.03 μM. | 23245570 | ||
| Sf9 | Function assay | Inhibition of human HER2 cytoplasmic domain (amino acids 676 to 1245) expressed in Sf9 cells by DELFIA time resolved fluorometry, IC50 = 0.16 μM. | 23245802 | ||
| A431 | Function assay | Inhibition of EGFR in human A431 cells by phosphotyrosine ELISA assay, IC50 = 0.0012 μM. | 24890652 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human ER-positive MCF7 cells, IC50 = 0.0012 μM. | 24890652 | ||
| U251 | Function assay | Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay, IC50 = 0.1247 μM. | 24890652 | ||
| MDA-MB-468 | Cytotoxicity assay | Cytotoxicity against human triple negative MDA-MB-468 cells, IC50 = 0.2352 μM. | 24890652 | ||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human triple negative MDA-MB-231 cells, IC50 = 0.4385 μM. | 24890652 | ||
| MDA-MB-435 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-435 cells, IC50 = 0.6221 μM. | 24890652 | ||
| Sf9 | Function assay | Inhibition of histidine-tagged recombinant EGFR cytoplasmic domain (amino acids 645-1186) (unknown origin) expressed in Sf9 cells assessed as reduction in enzyme autophosphorylation by DELFIA/time-resolved fluorometry, IC50 = 0.03 μM. | 25172421 | ||
| Sf9 | Function assay | Inhibition of histidine-tagged recombinant HER2 (unknown origin) expressed in Sf9 cells assessed as reduction in enzyme autophosphorylation by DELFIA/time-resolved fluorometry, IC50 = 0.2 μM. | 25172421 | ||
| FADU | Antiproliferative assay | Antiproliferative activity against human FADU cells, IC50 = 18 μM. | 26599532 | ||
| A549 | Function assay | Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA, IC50 = 0.011 μM. | 26756222 | ||
| Sf9 | Function assay | Inhibition of recombinant full-length GST-tagged human B-RAF V600E mutant (417 to 766 residues) expressed in Baculovirus infected Sf9 cells using N-terminal His-tagged human MEK1 as substrate by Nu-page gel-based phosphor screen analysis, IC50 = 0.06 μM. | 29549841 | ||
| Sf9 | Function assay | Inhibition of His-6 tagged recombinant EGFR cytoplasmic domain (645 to 1186 residues) (unknown origin) expressed in Baculovirus infected Sf9 cells by dissociation-enhanced lanthanide fluorescence immunoassay/time-resolved fluorometric analysis, IC50 = 0.08 μM. | 29549841 | ||
| HEK293 Flp-In | Function assay | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, Ki = 21 μM. | 22541068 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| NCI-H1648 | Growth Inhibition assay | Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50 = 0.04002 μM. | SANGER | ||
| TE-12 | Growth Inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50 = 0.05441 μM. | SANGER | ||
| ECC12 | Growth Inhibition assay | Inhibition of human ECC12 cell growth in a cell viability assay, IC50 = 0.08052 μM. | SANGER | ||
| BB30-HNC | Growth Inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50 = 0.14765 μM. | SANGER | ||
| LB996-RCC | Growth Inhibition assay | Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50 = 0.40161 μM. | SANGER | ||
| EW-24 | Growth Inhibition assay | Inhibition of human EW-24 cell growth in a cell viability assay, IC50 = 0.59443 μM. | SANGER | ||
| LC-1F | Growth Inhibition assay | Inhibition of human LC-1F cell growth in a cell viability assay, IC50 = 0.60632 μM. | SANGER | ||
| TK10 | Growth Inhibition assay | Inhibition of human TK10 cell growth in a cell viability assay, IC50 = 0.85878 μM. | SANGER | ||
| A388 | Growth Inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50 = 1.0938 μM. | SANGER | ||
| EKVX | Growth Inhibition assay | Inhibition of human EKVX cell growth in a cell viability assay, IC50 = 1.12354 μM. | SANGER | ||
| TE-9 | Growth Inhibition assay | Inhibition of human TE-9 cell growth in a cell viability assay, IC50 = 1.22511 μM. | SANGER | ||
| TE-1 | Growth Inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay, IC50 = 1.4048 μM. | SANGER | ||
| MOLT-16 | Growth Inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50 = 1.92925 μM. | SANGER | ||
| TE-6 | Growth Inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay, IC50 = 2.5678 μM. | SANGER | ||
| 697 | Growth Inhibition assay | Inhibition of human 697 cell growth in a cell viability assay, IC50 = 2.65305 μM. | SANGER | ||
| A253 | Growth Inhibition assay | Inhibition of human A253 cell growth in a cell viability assay, IC50 = 2.7516 μM. | SANGER | ||
| OS-RC-2 | Growth Inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50 = 2.94023 μM. | SANGER | ||
| KS-1 | Growth Inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay, IC50 = 2.94542 μM. | SANGER | ||
| MC116 | Growth Inhibition assay | Inhibition of human MC116 cell growth in a cell viability assay, IC50 = 3.62049 μM. | SANGER | ||
| LB2241-RCC | Growth Inhibition assay | Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50 = 3.81729 μM. | SANGER | ||
| RL95-2 | Growth Inhibition assay | Inhibition of human RL95-2 cell growth in a cell viability assay, IC50 = 4.0332 μM. | SANGER | ||
| HCE-T | Growth Inhibition assay | Inhibition of human HCE-T cell growth in a cell viability assay, IC50 = 4.10188 μM. | SANGER | ||
| NCCIT | Growth Inhibition assay | Inhibition of human NCCIT cell growth in a cell viability assay, IC50 = 4.38497 μM. | SANGER | ||
| GCIY | Growth Inhibition assay | Inhibition of human GCIY cell growth in a cell viability assay, IC50 = 4.63532 μM. | SANGER | ||
| LB1047-RCC | Growth Inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50 = 4.98379 μM. | SANGER | ||
| A3-KAW | Growth Inhibition assay | Inhibition of human A3-KAW cell growth in a cell viability assay, IC50 = 5.43946 μM. | SANGER | ||
| TE-15 | Growth Inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay, IC50 = 5.4727 μM. | SANGER | ||
| NOS-1 | Growth Inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50 = 5.49386 μM. | SANGER | ||
| EW-16 | Growth Inhibition assay | Inhibition of human EW-16 cell growth in a cell viability assay, IC50 = 6.25387 μM. | SANGER | ||
| LAMA-84 | Growth Inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50 = 7.00772 μM. | SANGER | ||
| TE-5 | Growth Inhibition assay | Inhibition of human TE-5 cell growth in a cell viability assay, IC50 = 7.04247 μM. | SANGER | ||
| HEL | Growth Inhibition assay | Inhibition of human HEL cell growth in a cell viability assay, IC50 = 7.33564 μM. | SANGER | ||
| NCI-H209 | Growth Inhibition assay | Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50 = 8.04412 μM. | SANGER | ||
| DJM-1 | Growth Inhibition assay | Inhibition of human DJM-1 cell growth in a cell viability assay, IC50 = 8.52964 μM. | SANGER | ||
| OVCAR-4 | Growth Inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50 = 8.84219 μM. | SANGER | ||
| NB17 | Growth Inhibition assay | Inhibition of human NB17 cell growth in a cell viability assay, IC50 = 9.25991 μM. | SANGER | ||
| SK-NEP-1 | Growth Inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50 = 9.35776 μM. | SANGER | ||
| NB5 | Growth Inhibition assay | Inhibition of human NB5 cell growth in a cell viability assay, IC50 = 10.29 μM. | SANGER | ||
| BV-173 | Growth Inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay, IC50 = 10.3272 μM. | SANGER | ||
| MPP-89 | Growth Inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay, IC50 = 10.442 μM. | SANGER | ||
| RPMI-6666 | Growth Inhibition assay | Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50 = 10.4969 μM. | SANGER | ||
| MS-1 | Growth Inhibition assay | Inhibition of human MS-1 cell growth in a cell viability assay, IC50 = 11.4658 μM. | SANGER | ||
| ALL-PO | Growth Inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50 = 11.5179 μM. | SANGER | ||
| NB10 | Growth Inhibition assay | Inhibition of human NB10 cell growth in a cell viability assay, IC50 = 11.7587 μM. | SANGER | ||
| NB13 | Growth Inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay, IC50 = 11.9914 μM. | SANGER | ||
| SCH | Growth Inhibition assay | Inhibition of human SCH cell growth in a cell viability assay, IC50 = 12.1891 μM. | SANGER | ||
| ES6 | Growth Inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay, IC50 = 12.475 μM. | SANGER | ||
| ETK-1 | Growth Inhibition assay | Inhibition of human ETK-1 cell growth in a cell viability assay, IC50 = 14.0885 μM. | SANGER | ||
| ES4 | Growth Inhibition assay | Inhibition of human ES4 cell growth in a cell viability assay, IC50 = 14.8445 μM. | SANGER | ||
| K-562 | Growth Inhibition assay | Inhibition of human K-562 cell growth in a cell viability assay, IC50 = 15.814 μM. | SANGER | ||
| D-502MG | Growth Inhibition assay | Inhibition of human D-502MG cell growth in a cell viability assay, IC50 = 17.3468 μM. | SANGER | ||
| LB647-SCLC | Growth Inhibition assay | Inhibition of human LB647-SCLC cell growth in a cell viability assay, IC50 = 17.7726 μM. | SANGER | ||
| TE-10 | Growth Inhibition assay | Inhibition of human TE-10 cell growth in a cell viability assay, IC50 = 18.1138 μM. | SANGER | ||
| MZ1-PC | Growth Inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50 = 18.3774 μM. | SANGER | ||
| CTB-1 | Growth Inhibition assay | Inhibition of human CTB-1 cell growth in a cell viability assay, IC50 = 18.5075 μM. | SANGER | ||
| NMC-G1 | Growth Inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50 = 18.8029 μM. | SANGER | ||
| C2BBe1 | Growth Inhibition assay | Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50 = 18.8664 μM. | SANGER | ||
| SK-PN-DW | Growth Inhibition assay | Inhibition of human SK-PN-DW cell growth in a cell viability assay, IC50 = 19.5482 μM. | SANGER | ||
| HCC2157 | Growth Inhibition assay | Inhibition of human HCC2157 cell growth in a cell viability assay, IC50 = 20.3361 μM. | SANGER | ||
| Becker | Growth Inhibition assay | Inhibition of human Becker cell growth in a cell viability assay, IC50 = 20.3541 μM. | SANGER | ||
| ST486 | Growth Inhibition assay | Inhibition of human ST486 cell growth in a cell viability assay, IC50 = 20.4093 μM. | SANGER | ||
| LC-2-ad | Growth Inhibition assay | Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50 = 20.9637 μM. | SANGER | ||
| NCI-H747 | Growth Inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50 = 21.5139 μM. | SANGER | ||
| BE-13 | Growth Inhibition assay | Inhibition of human BE-13 cell growth in a cell viability assay, IC50 = 21.8158 μM. | SANGER | ||
| no-11 | Growth Inhibition assay | Inhibition of human no-11 cell growth in a cell viability assay, IC50 = 21.9106 μM. | SANGER | ||
| TE-8 | Growth Inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay, IC50 = 22.6318 μM. | SANGER | ||
| NB6 | Growth Inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay, IC50 = 22.8303 μM. | SANGER | ||
| BB65-RCC | Growth Inhibition assay | Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50 = 22.9623 μM. | SANGER | ||
| SK-UT-1 | Growth Inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50 = 23.1497 μM. | SANGER | ||
| D-392MG | Growth Inhibition assay | Inhibition of human D-392MG cell growth in a cell viability assay, IC50 = 24.2934 μM. | SANGER | ||
| JVM-2 | Growth Inhibition assay | Inhibition of human JVM-2 cell growth in a cell viability assay, IC50 = 24.5333 μM. | SANGER | ||
| SW954 | Growth Inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50 = 24.5916 μM. | SANGER | ||
| QIMR-WIL | Growth Inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50 = 25.1973 μM. | SANGER | ||
| MEG-01 | Growth Inhibition assay | Inhibition of human MEG-01 cell growth in a cell viability assay, IC50 = 25.9016 μM. | SANGER | ||
| A101D | Growth Inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50 = 28.7139 μM. | SANGER | ||
| LB831-BLC | Growth Inhibition assay | Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50 = 30.4004 μM. | SANGER | ||
| KGN | Growth Inhibition assay | Inhibition of human KGN cell growth in a cell viability assay, IC50 = 30.8661 μM. | SANGER | ||
| HC-1 | Growth Inhibition assay | Inhibition of human HC-1 cell growth in a cell viability assay, IC50 = 31.3508 μM. | SANGER | ||
| CP66-MEL | Growth Inhibition assay | Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50 = 31.8366 μM. | SANGER | ||
| D-542MG | Growth Inhibition assay | Inhibition of human D-542MG cell growth in a cell viability assay, IC50 = 32.4337 μM. | SANGER | ||
| LS-513 | Growth Inhibition assay | Inhibition of human LS-513 cell growth in a cell viability assay, IC50 = 33.4844 μM. | SANGER | ||
| DOHH-2 | Growth Inhibition assay | Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50 = 33.6589 μM. | SANGER | ||
| NB69 | Growth Inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50 = 33.9206 μM. | SANGER | ||
| SW962 | Growth Inhibition assay | Inhibition of human SW962 cell growth in a cell viability assay, IC50 = 35.7217 μM. | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition assay | Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay, IC50 = 36.0724 μM. | SANGER | ||
| MONO-MAC-6 | Growth Inhibition assay | Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50 = 36.5359 μM. | SANGER | ||
| MLMA | Growth Inhibition assay | Inhibition of human MLMA cell growth in a cell viability assay, IC50 = 38.652 μM. | SANGER | ||
| HOP-62 | Growth Inhibition assay | Inhibition of human HOP-62 cell growth in a cell viability assay, IC50 = 39.1765 μM. | SANGER | ||
| LP-1 | Growth Inhibition assay | Inhibition of human LP-1 cell growth in a cell viability assay, IC50 = 39.4415 μM. | SANGER | ||
| ONS-76 | Growth Inhibition assay | Inhibition of human ONS-76 cell growth in a cell viability assay, IC50 = 39.9152 μM. | SANGER | ||
| KNS-42 | Growth Inhibition assay | Inhibition of human KNS-42 cell growth in a cell viability assay, IC50 = 40.0531 μM. | SANGER | ||
| NCI-H1581 | Growth Inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50 = 41.1842 μM. | SANGER | ||
| DSH1 | Growth Inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay, IC50 = 42.407 μM. | SANGER | ||
| NCI-H1355 | Growth Inhibition assay | Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50 = 42.839 μM. | SANGER | ||
| D-247MG | Growth Inhibition assay | Inhibition of human D-247MG cell growth in a cell viability assay, IC50 = 45.719 μM. | SANGER | ||
| MC-CAR | Growth Inhibition assay | Inhibition of human MC-CAR cell growth in a cell viability assay, IC50 = 45.9691 μM. | SANGER | ||
| EW-1 | Growth Inhibition assay | Inhibition of human EW-1 cell growth in a cell viability assay, IC50 = 47.5624 μM. | SANGER | ||
| GI-ME-N | Growth Inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50 = 48.1384 μM. | SANGER | ||
| BT-474 | Growth Inhibition assay | Inhibition of human BT-474 cell growth in a cell viability assay, IC50 = 48.1738 μM. | SANGER | ||
| LB373-MEL-D | Growth Inhibition assay | Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50 = 48.7563 μM. | SANGER | ||
| BHT-101 | Growth Inhibition assay | Inhibition of human BHT-101 cell growth in a cell viability assay, IC50 = 22.0629 μM. | SANGER | ||
| OVCAR-4 | Growth Inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50 = 22.47 μM. | SANGER | ||
| SW1573 | Growth Inhibition assay | Inhibition of human SW1573 cell growth in a cell viability assay, IC50 = 22.7934 μM. | SANGER | ||
| CHL-1 | Growth Inhibition assay | Inhibition of human CHL-1 cell growth in a cell viability assay, IC50 = 23.2833 μM. | SANGER | ||
| BFTC-905 | Growth Inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50 = 23.2892 μM. | SANGER | ||
| TE-12 | Growth Inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50 = 23.5782 μM. | SANGER | ||
| NCI-H358 | Growth Inhibition assay | Inhibition of human NCI-H358 cell growth in a cell viability assay, IC50 = 23.6477 μM. | SANGER | ||
| OVCAR-5 | Growth Inhibition assay | Inhibition of human OVCAR-5 cell growth in a cell viability assay, IC50 = 24.104 μM. | SANGER | ||
| CGTH-W-1 | Growth Inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50 = 25.0804 μM. | SANGER | ||
| SNU-423 | Growth Inhibition assay | Inhibition of human SNU-423 cell growth in a cell viability assay, IC50 = 25.366 μM. | SANGER | ||
| CP50-MEL-B | Growth Inhibition assay | Inhibition of human CP50-MEL-B cell growth in a cell viability assay, IC50 = 25.7399 μM. | SANGER | ||
| NCI-H2087 | Growth Inhibition assay | Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50 = 25.8655 μM. | SANGER | ||
| RMG-I | Growth Inhibition assay | Inhibition of human RMG-I cell growth in a cell viability assay, IC50 = 25.9219 μM. | SANGER | ||
| KP-N-YS | Growth Inhibition assay | Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50 = 26.202 μM. | SANGER | ||
| OMC-1 | Growth Inhibition assay | Inhibition of human OMC-1 cell growth in a cell viability assay, IC50 = 26.508 μM. | SANGER | ||
| DMS-114 | Growth Inhibition assay | Inhibition of human DMS-114 cell growth in a cell viability assay, IC50 = 27.3966 μM. | SANGER | ||
| SHP-77 | Growth Inhibition assay | Inhibition of human SHP-77 cell growth in a cell viability assay, IC50 = 27.488 μM. | SANGER | ||
| MPP-89 | Growth Inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay, IC50 = 27.9438 μM. | SANGER | ||
| NCI-H1581 | Growth Inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50 = 28.4535 μM. | SANGER | ||
| D-283MED | Growth Inhibition assay | Inhibition of human D-283MED cell growth in a cell viability assay, IC50 = 28.4674 μM. | SANGER | ||
| MOLT-4 | Growth Inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50 = 28.9072 μM. | SANGER | ||
| ES6 | Growth Inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay, IC50 = 29.6436 μM. | SANGER | ||
| NB6 | Growth Inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay, IC50 = 29.8638 μM. | SANGER | ||
| SW954 | Growth Inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50 = 29.9407 μM. | SANGER | ||
| A388 | Growth Inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50 = 29.9422 μM. | SANGER | ||
| OAW-28 | Growth Inhibition assay | Inhibition of human OAW-28 cell growth in a cell viability assay, IC50 = 30.2278 μM. | SANGER | ||
| SK-MES-1 | Growth Inhibition assay | Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50 = 31.2208 μM. | SANGER | ||
| NCI-H441 | Growth Inhibition assay | Inhibition of human NCI-H441 cell growth in a cell viability assay, IC50 = 31.9868 μM. | SANGER | ||
| HOP-92 | Growth Inhibition assay | Inhibition of human HOP-92 cell growth in a cell viability assay, IC50 = 32.2356 μM. | SANGER | ||
| NB14 | Growth Inhibition assay | Inhibition of human NB14 cell growth in a cell viability assay, IC50 = 32.7251 μM. | SANGER | ||
| MS-1 | Growth Inhibition assay | Inhibition of human MS-1 cell growth in a cell viability assay, IC50 = 32.7604 μM. | SANGER | ||
| YKG-1 | Growth Inhibition assay | Inhibition of human YKG-1 cell growth in a cell viability assay, IC50 = 32.8336 μM. | SANGER | ||
| SiHa | Growth Inhibition assay | Inhibition of human SiHa cell growth in a cell viability assay, IC50 = 33.3829 μM. | SANGER | ||
| HAL-01 | Growth Inhibition assay | Inhibition of human HAL-01 cell growth in a cell viability assay, IC50 = 34.2376 μM. | SANGER | ||
| Ca-Ski | Growth Inhibition assay | Inhibition of human Ca-Ski cell growth in a cell viability assay, IC50 = 34.7669 μM. | SANGER | ||
| NCI-H747 | Growth Inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50 = 34.9875 μM. | SANGER | ||
| KYSE-510 | Growth Inhibition assay | Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50 = 35.6485 μM. | SANGER | ||
| A204 | Growth Inhibition assay | Inhibition of human A204 cell growth in a cell viability assay, IC50 = 35.7209 μM. | SANGER | ||
| HSC-3 | Growth Inhibition assay | Inhibition of human HSC-3 cell growth in a cell viability assay, IC50 = 36.0086 μM. | SANGER | ||
| HuP-T3 | Growth Inhibition assay | Inhibition of human HuP-T3 cell growth in a cell viability assay, IC50 = 36.4832 μM. | SANGER | ||
| RPMI-8226 | Growth Inhibition assay | Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50 = 36.6208 μM. | SANGER | ||
| QIMR-WIL | Growth Inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50 = 36.644 μM. | SANGER | ||
| HuH-7 | Growth Inhibition assay | Inhibition of human HuH-7 cell growth in a cell viability assay, IC50 = 38.6184 μM. | SANGER | ||
| CAL-12T | Growth Inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50 = 38.9416 μM. | SANGER | ||
| GT3TKB | Growth Inhibition assay | Inhibition of human GT3TKB cell growth in a cell viability assay, IC50 = 39.1921 μM. | SANGER | ||
| OC-314 | Growth Inhibition assay | Inhibition of human OC-314 cell growth in a cell viability assay, IC50 = 39.7125 μM. | SANGER | ||
| NCI-H2228 | Growth Inhibition assay | Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50 = 40.1403 μM. | SANGER | ||
| NCI-H727 | Growth Inhibition assay | Inhibition of human NCI-H727 cell growth in a cell viability assay, IC50 = 40.2531 μM. | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50 = 40.4706 μM. | SANGER | ||
| MMAC-SF | Growth Inhibition assay | Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50 = 40.9235 μM. | SANGER | ||
| HTC-C3 | Growth Inhibition assay | Inhibition of human HTC-C3 cell growth in a cell viability assay, IC50 = 41.4169 μM. | SANGER | ||
| SF295 | Growth Inhibition assay | Inhibition of human SF295 cell growth in a cell viability assay, IC50 = 41.5379 μM. | SANGER | ||
| U-2-OS | Growth Inhibition assay | Inhibition of human U-2-OS cell growth in a cell viability assay, IC50 = 41.8567 μM. | SANGER | ||
| HPAF-II | Growth Inhibition assay | Inhibition of human HPAF-II cell growth in a cell viability assay, IC50 = 41.9382 μM. | SANGER | ||
| KYSE-450 | Growth Inhibition assay | Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50 = 42.4707 μM. | SANGER | ||
| DMS-273 | Growth Inhibition assay | Inhibition of human DMS-273 cell growth in a cell viability assay, IC50 = 43.2836 μM. | SANGER | ||
| HT-1376 | Growth Inhibition assay | Inhibition of human HT-1376 cell growth in a cell viability assay, IC50 = 43.3156 μM. | SANGER | ||
| 786-0 | Growth Inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50 = 43.6261 μM. | SANGER | ||
| NCI-H810 | Growth Inhibition assay | Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50 = 44.0136 μM. | SANGER | ||
| 8305C | Growth Inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50 = 44.645 μM. | SANGER | ||
| DSH1 | Growth Inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay, IC50 = 45.7042 μM. | SANGER | ||
| KYSE-520 | Growth Inhibition assay | Inhibition of human KYSE-520 cell growth in a cell viability assay, IC50 = 46.5721 μM. | SANGER | ||
| TYK-nu | Growth Inhibition assay | Inhibition of human TYK-nu cell growth in a cell viability assay, IC50 = 46.7092 μM. | SANGER | ||
| EPLC-272H | Growth Inhibition assay | Inhibition of human EPLC-272H cell growth in a cell viability assay, IC50 = 46.7283 μM. | SANGER | ||
| T-24 | Growth Inhibition assay | Inhibition of human T-24 cell growth in a cell viability assay, IC50 = 47.9292 μM. | SANGER | ||
| BHY | Growth Inhibition assay | Inhibition of human BHY cell growth in a cell viability assay, IC50 = 47.999 μM. | SANGER | ||
| NCI-H82 | Growth Inhibition assay | Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50 = 48.217 μM. | SANGER | ||
| SF268 | Growth Inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay, IC50 = 48.6189 μM. | SANGER | ||
| C-33-A | Growth Inhibition assay | Inhibition of human C-33-A cell growth in a cell viability assay, IC50 = 48.7554 μM. | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition assay | Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50 = 48.8388 μM. | SANGER | ||
| HCC1954 | Growth Inhibition assay | Inhibition of human HCC1954 cell growth in a cell viability assay, IC50 = 49.0871 μM. | SANGER | ||
| NCI-H1666 | Growth Inhibition assay | Inhibition of human NCI-H1666 cell growth in a cell viability assay, IC50 = 49.3642 μM. | SANGER | ||
| GR-ST | Growth Inhibition assay | Inhibition of human GR-ST cell growth in a cell viability assay, IC50 = 49.3695 μM. | SANGER | ||
| Ca9-22 | Growth Inhibition assay | Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50 = 49.4013 μM. | SANGER | ||
| D-502MG | Growth Inhibition assay | Inhibition of human D-502MG cell growth in a cell viability assay, IC50 = 49.417 μM. | SANGER | ||
| SCC-4 | Growth Inhibition assay | Inhibition of human SCC-4 cell growth in a cell viability assay, IC50 = 49.5602 μM. | SANGER | ||
| RKO | Growth Inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50 = 49.8356 μM. | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Erlotinib是一种EGFR抑制剂，IC50 为 2 nM，对EGFR的敏感性比对人c-Src 或 v-Ab高1000多倍。Erlotinib可诱导自噬。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Erlotinib HCl有效抑制完整细胞，包括HNS人头颈部肿瘤细胞(IC50 20nM)，DiFi人结肠癌细胞和MDA MB-468人乳腺癌细胞中EGFR活化。Erlotinib HCl (1 μM)在DiFi人结肠癌细胞中诱导细胞凋亡。[1] Erlotinib抑制一组NSCLC细胞系，包括A549，H322，H3255，H358，H661，H1650，H1975，H1299，H596的生长，IC50范围为29 nM到>20 μM。[2] Erlotinib HCl(2 μM)显著抑制AsPC-1和BxPC-3胰细胞生长。[3] Erlotinib HCl与gemcitabine结合使用，在KRAS突变的胰腺癌细胞中具有协同作用。10微摩尔Erlotinib HCl抑制Y845 (Src依赖性磷酸化)和Y1068 (自身磷酸化)位点的EGFR磷酸化。[4]结合Erlotinib HCl能够下调rapamycin刺激的Akt活性，并产生协同的细胞生长抑制作用。[5] |
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|---|---|---|---|---|
| 激酶实验 | 激酶试验 | |||
| 96孔板与100 μL/孔0.25 mg/mL PGT的PBS溶液在37℃下培养过夜进行涂层。过量PGT通过抽吸移除，板用洗涤缓冲液(0.1% Tween 20的PBS溶液)清洗3次。激酶反应在50 μL 50 mM HEPES (pH 7.3)中进行，反应液中包含125 mM 氯化钠，24 mM氯化镁，0.1 mM 原钒酸钠，20 μM ATP，1.6 μg/mL EGF，和15 ng从A431细胞膜亲和纯化的EGFR。加入Erlotinib HCl的DMSO溶液，终DMSO浓度为2.5%。磷酸化作用通过加入ATP起始，并在室温下恒定振荡进行8分钟。激酶反应通过抽吸反应混合物终止，并用洗涤缓冲液清洗4次。磷酸化的PGT通过与50 μL/孔HRP偶联的PY54抗磷酸酪氨酸抗体(在封闭缓冲液(3% BSA和0.05% Tween 20的PBS溶液)中稀释为0.2 μg/mL)培育25分钟进行测量。通过抽吸移除抗体，将板用洗涤缓冲液清洗4次。比色信号通过加入50μL /孔TMB微孔过氧化物酶底物产生，通过加入50 μL/孔0.09 M硫酸停止。磷酸酪氨酸通过测量450 nm下吸光度进行估计。对照组信号通常为0.6-1.2吸收单元，没有AlP，EGFR，或PGT的孔中基本上没有背景干扰，并且该信号与10分钟的培养时间成比例。 | ||||
| 细胞实验 | 细胞系 | A549，H322，H3255，H358 H661，H1650，H1975，H1299，H596 细胞 | ||
| 浓度 | 30 nM-20 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 以指数生长的细胞以一式三份接种在96孔塑料板，并暴露于连续稀释的erlotinib，pemetrexed，或4:1固定浓度比的结合物，培养72小时。细胞活性通过细胞计数和MTT法测定。生长抑制表示为药物处理组与PBS处理的对照组细胞(认为100%存活)中存活细胞的百分比。IC50值是与未处理的对照组细胞相比，在药物中暴露72小时，导致50%细胞生长抑制的浓度，通过CalcuSyn软件计算。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Cleaved PARP / PARP P-Raf-1 / t-Raf-1 / p-MEK / t-MEK / p-ERK / t-ERK / p-PI3K / t-PI3K / p-AKT / AKT p-STAT3 / STAT3 / PTPMeg2 / p-EGFR / EGFR / pJAK2 / JAK2 / Bcl2 / Bcl-xl / Survivin |
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27508092 | |
| Immunofluorescence | β-catenin E-cadherin / Vimentin |
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25209444 | |
| Growth inhibition assay | Cell viability IC50 |
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30377412 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在100 mg/kg剂量下，Erlotinib HCl完全防止EGF诱导的异种移植人HN5肿瘤的无胸腺小鼠体内EGFR自身磷酸化，和治疗小鼠的肝EGFR自身磷酸化。[1] Erlotinib HCl (100 mg/Kg)抑制H460a和A549肿瘤模型，分别具有71和93%的抑制率。[5] |
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|---|---|---|
| 动物实验 | Animal Models | 负荷HPAC细胞的雄性5周大的BALB-nu/nu小鼠 |
| Dosages | 50 mg/kg | |
| Administration | 口服给药 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04172779 | Not yet recruiting | Cirrhosis Liver |
University of Texas Southwestern Medical Center|National Cancer Institute (NCI) |
July 2024 | Phase 2 |
| NCT06161558 | Not yet recruiting | Neoplasms |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
May 15 2024 | Phase 1 |
| NCT05827614 | Recruiting | Non-small Cell Lung Cancer|Non-Small Cell Lung Adenocarcinoma|Non-Small Cell Squamous Lung Cancer|Head and Neck Squamous Cell Carcinoma|Esophageal Cancer|Gastric Cancer|Breast Cancer|Bladder Cancer|Ovarian Cancer|Endometrial Cancer|Liposarcoma |
Boundless Bio |
March 24 2023 | Phase 1 |
| NCT03460678 | Terminated | Carcinoma Non-Small-Cell Lung |
Hikma Pharmaceuticals LLC |
February 28 2018 | Phase 4 |
化学信息&溶解度
| 分子量 | 393.44 | 分子式 | C22H23N3O4 |
| CAS号 | 183321-74-6 | SDF | Download Erlotinib SDF |
| Smiles | COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 100 mg/mL ( (254.16 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 11 mg/mL (27.95 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
Can you please give me some advice for which solvent we should use to dissolve it for animal studies?
回答：
For in vivo application, we recommend to use 5% DMSO+45% PEG 300+ddH2O up to 6mg/ml.
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