Lapatinib
别名: GSK572016, GW2016 中文名称：拉帕替尼
Lapatinib，以 Lapatinib Ditosylate的形式使用，是一种有效的EGFR和ErbB2抑制剂，在无细胞试验中IC50分别为10.2和9.8 nM。Lapatinib 可诱导 ferroptosis 和细胞自噬。
Lapatinib Chemical Structure
CAS: 231277-92-2
产品质控
批次：
纯度：
99.95%
99.95
常与Lapatinib一起在实验中被使用的化合物
Lapatinib和Gefitinib通过下调SK-Br-3HER2扩增乳腺癌细胞系中拓扑异构酶IIα的表达来诱导耐药性。
Afatinib通过诱导G1细胞周期停滞和凋亡，在体外比Lapatinib更有效地抑制GLM-1和GLM-1HerR2细胞的生长。
Lapatinib和吉西他滨在HER2阳性乳腺癌细胞中表现出协同抗肿瘤作用。
Lapatinib和Paclitaxel的使用在食管鳞癌中表现出更好的抗肿瘤功效。
Guo XF, et al. Cancer Chemother Pharmacol. 2018;82(3):383-394.
Lapatinib和Erlotinib通过抑制药物流出功能逆转MRP7介导的多药耐药性。
Lapatinib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 |
|---|---|---|---|---|---|
| A431 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 |
| A431 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 |
| BT474 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 |
| BT474 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 |
| A431 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER1 phosphorylation (unknown origin) expressed in human A431 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 |
| BT474 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER2 phosphorylation (unknown origin) expressed in human BT474 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of HER2 delta16 mutant autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting | 24355130 |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting | 24355130 |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2delta16 at 10 uM after 2 hrs by Western blotting | 24355130 |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2 at 10 uM after 2 hrs by Western blotting | 24355130 |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting | 24355130 |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting | 24355130 |
| A549 | Function assay | 50 uM | 2 hrs | Inhibition of EGFR phosphorylation at Y1068 in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method | 28238614 |
| A549 | Function assay | 50 uM | 2 hrs | Inhibition of EGFR phosphorylation at Tyr residue in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method | 28238614 |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, IC50 = 0.011 μM. | 25151582 | |
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.017 μM. | 19028425 | |
| BT474 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method, IC50 = 0.025 μM. | 21887403 | |
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.029 μM. | 19888761 | |
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay, IC50 = 0.029 μM. | 22372864 | |
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0301 μM. | 25305330 | |
| BT474 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay, IC50 = 0.031 μM. | 27288180 | |
| CAL27 | Function assay | 16 hrs | Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot, IC50 = 0.032 μM. | 21080629 | |
| NCI-N87 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay, IC50 = 0.036 μM. | 22372864 | |
| insect cells | Function assay | 5 mins | Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.03755 μM. | 30096580 | |
| MDA-MB-175 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-175 cells expressing Src, Ret and low HER-2 after 72 hrs by SRB assay, IC50 = 0.0444 μM. | 22372864 | |
| SK-BR-3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.06 μM. | 27769671 | |
| BT474 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0639 μM. | 25305330 | |
| NCI-N87 | Antiproliferative assay | 3 days | Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining, IC50 = 0.09 μM. | 22101132 | |
| BT474 | Antiproliferative assay | 3 days | Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining, IC50 = 0.1 μM. | 22101132 | |
| Calu3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay, IC50 = 0.1 μM. | 28092860 | |
| BT474 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.1 μM. | 27769671 | |
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50 = 0.104 μM. | 19888761 | |
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay, IC50 = 0.104 μM. | 22372864 | |
| HeLa | Antiproliferative assay | 12 hrs | Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay, IC50 = 0.12 μM. | 26652482 | |
| A431 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.15 μM. | 27769671 | |
| MDA-MB-453 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.19 μM. | 25305330 | |
| BT474 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 0.2 μM. | 29089259 | |
| B16F10 | Antiproliferative assay | 12 hrs | Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay, IC50 = 0.21 μM. | 26652482 | |
| Sf21 | Function assay | 5 mins | Inhibition of N-terminal GST-tagged recombinant human EGFR T790M mutant expressed in baculovirus infected Sf21 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.22489 μM. | 30096580 | |
| Calu3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.23 μM. | 25305330 | |
| DIFI | Cytotoxicity assay | 4 days | Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.235 μM. | 22169601 | |
| HepG2 | Antiproliferative assay | 12 hrs | Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay, IC50 = 0.27 μM. | 26652482 | |
| EOL-1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 0.41 μM. | 29089259 | |
| MCF7 | Antiproliferative assay | 12 hrs | Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay, IC50 = 0.47 μM. | 26652482 | |
| SKBR3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay, IC50 = 0.49 μM. | 27187856 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.51 μM. | 27769671 | |
| CAL27 | Cytotoxicity assay | 4 days | Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.53 μM. | 22169601 | |
| MDA-MB-453 | Cytotoxicity assay | 72 hrs | Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay, IC50 = 0.555 μM. | 22372864 | |
| SKOV3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.59 μM. | 25305330 | |
| HCC827 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay, IC50 = 0.6 μM. | 29421573 | |
| A431NS | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431NS cells after 72 hrs by MTT assay, IC50 = 0.6 μM. | 28092860 | |
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.6431 μM. | 25305330 | |
| BT474 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay, GI50 = 0.93 μM. | 26475520 | |
| MDA-MB-361 | Cytotoxicity assay | 72 hrs | Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay, IC50 = 1.029 μM. | 22372864 | |
| GXF251L | Cytotoxicity assay | 4 days | Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 1.48 μM. | 22169601 | |
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.6 μM. | 22595177 | |
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.62 μM. | 22182581 | |
| LXFA 629L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 629L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.87 μM. | 22169601 | |
| DU145 | Cytotoxicity assay | 4 days | Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.99 μM. | 22169601 | |
| SKOV3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay, IC50 = 2.99 μM. | 22182581 | |
| NCI-H1781 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-H1781 cells expressing HER-2 G776insV_G/C after 72 hrs by SRB assay, IC50 = 3.047 μM. | 22372864 | |
| OVXF 899L | Cytotoxicity assay | 4 days | Cytotoxicity against human OVXF 899L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.35 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 = 3.51 μM. | 22169601 | |
| LNCAP | Cytotoxicity assay | 4 days | Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.68 μM. | 22169601 | |
| Bel7402 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50 = 3.7 μM. | 28092860 | |
| LXFA 526L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 526L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.21 μM. | 22169601 | |
| NIH/3T3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay, IC50 = 4.3 μM. | 22595177 | |
| UXF 1138L | Cytotoxicity assay | 4 days | Cytotoxicity against human UXF 1138L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.4 μM. | 22169601 | |
| SK-BR-3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay, IC50 = 4.4 μM. | 28092860 | |
| PC3M | Cytotoxicity assay | 4 days | Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.55 μM. | 22169601 | |
| COLO205 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay, IC50 = 4.6 μM. | 28092860 | |
| HT-29 | Cytotoxicity assay | 4 days | Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.62 μM. | 22169601 | |
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM. | 29421573 | |
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM. | 28711703 | |
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 4.8 μM. | 28238614 | |
| MCF7 | Cytotoxicity assay | 4 days | Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.83 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 = 4.85 μM. | 22169601 | |
| MCF7 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay, IC50 = 5.02 μM. | 30096580 | |
| SKBR3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay, IC50 = 5.05 μM. | 23927972 | |
| SKHEP1 | Antiproliferative assay | hrs | Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay, IC50 = 5.3 μM. | 20143778 | |
| RKO | Cytotoxicity assay | 4 days | Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.35 μM. | 22169601 | |
| MDA-MB-231 | Antiproliferative assay | hrs | Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay, IC50 = 5.4 μM. | 20143778 | |
| Hep3B2 | Antiproliferative assay | hrs | Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay, IC50 = 5.49 μM. | 20143778 | |
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 5.7 μM. | 29089259 | |
| LXFA 289L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 289L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.79 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 = 5.8 μM. | 22169601 | |
| HCT116 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay, IC50 = 5.92 μM. | 30096580 | |
| 22Rv1 | Cytotoxicity assay | 4 days | Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.06 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 = 6.12 μM. | 22169601 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 6.2 μM. | 28092860 | |
| NCI-H522 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay, IC50 = 6.4 μM. | 28092860 | |
| MCF7 | Antiproliferative assay | hrs | Antiproliferative activity against human MCF7 cells after hrs by ATP content assay, IC50 = 6.6 μM. | 20143778 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 6.74 μM. | 27187856 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 6.8 μM. | 29684708 | |
| PXF 1118L | Cytotoxicity assay | 4 days | Cytotoxicity against human PXF 1118L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.86 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 = 7.18 μM. | 22169601 | |
| RXF 1781L | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 1781L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.67 μM. | 22169601 | |
| MDA231 | Cytotoxicity assay | 4 days | Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.7 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 = 7.73 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 = 7.77 μM. | 22169601 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 8.1 μM. | 29089259 | |
| PANC1 | Cytotoxicity assay | 4 days | Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.12 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 = 8.36 μM. | 22169601 | |
| NCI-H460 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 8.4 μM. | 28092860 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 8.468 μM. | 25305330 | |
| NCI-H1975 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50 = 9.08 μM. | 28711703 | |
| NCI-H1975 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 9.08 μM. | 28238614 | |
| RXF 486L | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 486L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.1 μM. | 22169601 | |
| Saos2 | Cytotoxicity assay | 4 days | Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.38 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 = 9.46 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 = 9.49 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 = 9.65 μM. | 22169601 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 10.12 μM. | 29684708 | |
| MEXF 462NL | Cytotoxicity assay | 4 days | Cytotoxicity against human MEXF 462NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.13 μM. | 22169601 | |
| A2780 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50 = 10.4 μM. | 29684708 | |
| TE671 | Cytotoxicity assay | 4 days | Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.95 μM. | 22169601 | |
| RAW264.7 | Antileishmanial assay | 96 hrs | Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay, EC50 = 11 μM. | 28337329 | |
| PAXF 1657L | Cytotoxicity assay | 4 days | Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.11 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 = 11.37 μM. | 22169601 | |
| MKN45 | Cytotoxicity assay | 4 days | Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.48 μM. | 22169601 | |
| BXF 1352L | Cytotoxicity assay | 4 days | Cytotoxicity against human BXF 1352L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.53 μM. | 22169601 | |
| HepG2 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay, IC50 = 11.71 μM. | 30096580 | |
| BXF 1218L | Cytotoxicity assay | 4 days | Cytotoxicity against human BXF 1218L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.77 μM. | 22169601 | |
| Caco | Cytotoxicity assay | 24 hrs | Cytotoxicity against human Caco cells after 24 hrs by SRB assay, IC50 = 12.11 μM. | 30096580 | |
| SW480 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM. | 29421573 | |
| SW480 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM. | 28711703 | |
| SW480 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SW480 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 12.58 μM. | 28238614 | |
| NCI-H1975 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50 = 12.68 μM. | 29421573 | |
| 3T3 | Antitrypanosomal assay | 48 hrs | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay, EC50 = 13 μM. | 28337329 | |
| HCT116 | Cytotoxicity assay | 4 days | Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.14 μM. | 22169601 | |
| OVCAR3 | Cytotoxicity assay | 4 days | Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.44 μM. | 22169601 | |
| H460 | Cytotoxicity assay | 4 days | Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.46 μM. | 22169601 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay, IC50 = 14.9 μM. | 29421573 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay, IC50 = 14.9 μM. | 28711703 | |
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 14.9 μM. | 28238614 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 15.71 μM. | 24355130 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 15.79 μM. | 24355130 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 19.22 μM. | 24355130 | |
| MDA-MB-468 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay, IC50 = 20 μM. | 28092860 | |
| HCC827 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 22.3 μM. | 29089259 | |
| ETK-1 | Growth Inhibition Assay | IC50=10.623 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=10.2565 μM | SANGER | ||
| TE-15 | Growth Inhibition Assay | IC50=10.245 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=9.98291 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=9.96307 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=9.66287 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=9.5742 μM | SANGER | ||
| D-336MG | Growth Inhibition Assay | IC50=9.47395 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=9.11675 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=7.76159 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=7.48894 μM | SANGER | ||
| EVSA-T | Growth Inhibition Assay | IC50=7.42811 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=7.22744 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=7.07183 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=6.51682 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=6.43694 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=6.26561 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=6.21001 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=5.80046 μM | SANGER | ||
| COLO-668 | Growth Inhibition Assay | IC50=5.72667 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=5.39245 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=5.02159 μM | SANGER | ||
| UACC-812 | Growth Inhibition Assay | IC50=4.56153 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=4.16522 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=4.0373 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=3.55356 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=3.54501 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=3.46975 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=3.40041 μM | SANGER | ||
| RL95-2 | Growth Inhibition Assay | IC50=3.1567 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=2.0483 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=1.99199 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=1.97335 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=1.55201 μM | SANGER | ||
| LC-1F | Growth Inhibition Assay | IC50=1.38244 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=1.36228 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.02544 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=0.05326 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=0.0574 μM | SANGER | ||
| ECC12 | Growth Inhibition Assay | IC50=0.09231 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=0.09396 μM | SANGER | ||
| BT-474 | Growth Inhibition Assay | IC50=0.21315 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=0.24654 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=0.44874 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=0.49057 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=0.72258 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=0.74453 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=1.15403 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=10.961 μM | SANGER | ||
| KNS-42 | Growth Inhibition Assay | IC50=11.7255 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=12.1712 μM | SANGER | ||
| SR | Growth Inhibition Assay | IC50=12.2064 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=12.8985 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=13.078 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=13.2577 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=13.6428 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=14.2374 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=14.5145 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=14.7889 μM | SANGER | ||
| CA46 | Growth Inhibition Assay | IC50=15.0586 μM | SANGER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=15.1901 μM | SANGER | ||
| BC-1 | Growth Inhibition Assay | IC50=15.3314 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=15.8173 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=16.0924 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=16.7313 μM | SANGER | ||
| LB647-SCLC | Growth Inhibition Assay | IC50=16.9372 μM | SANGER | ||
| NCI-H1694 | Growth Inhibition Assay | IC50=17.1529 μM | SANGER | ||
| NCI-H322M | Growth Inhibition Assay | IC50=17.4366 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=18.3914 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=18.4386 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=18.7409 μM | SANGER | ||
| RPMI-8402 | Growth Inhibition Assay | IC50=19.0742 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=20.2344 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=20.8587 μM | SANGER | ||
| MRK-nu-1 | Growth Inhibition Assay | IC50=20.913 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=21.038 μM | SANGER | ||
| NALM-6 | Growth Inhibition Assay | IC50=21.1967 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=21.4813 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=22.1402 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=22.2149 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=22.3965 μM | SANGER | ||
| SKM-1 | Growth Inhibition Assay | IC50=22.7351 μM | SANGER | ||
| DMS-153 | Growth Inhibition Assay | IC50=23.4204 μM | SANGER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=23.5452 μM | SANGER | ||
| LP-1 | Growth Inhibition Assay | IC50=23.8097 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=24.292 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=25.2036 μM | SANGER | ||
| U-698-M | Growth Inhibition Assay | IC50=25.2503 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=25.6418 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=25.673 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=26.273 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=26.3369 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=26.5181 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=26.7575 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=27.3867 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=27.4566 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=28.1446 μM | SANGER | ||
| TE-441-T | Growth Inhibition Assay | IC50=28.789 μM | SANGER | ||
| EW-24 | Growth Inhibition Assay | IC50=29.1259 μM | SANGER | ||
| no-10 | Growth Inhibition Assay | IC50=29.1631 μM | SANGER | ||
| D-542MG | Growth Inhibition Assay | IC50=29.9221 μM | SANGER | ||
| ST486 | Growth Inhibition Assay | IC50=30.6451 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=30.8057 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=31.5972 μM | SANGER | ||
| BL-41 | Growth Inhibition Assay | IC50=32.1054 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=32.3855 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=32.4967 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=32.7751 μM | SANGER | ||
| MFH-ino | Growth Inhibition Assay | IC50=34.3224 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=34.6748 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=35.3667 μM | SANGER | ||
| EB2 | Growth Inhibition Assay | IC50=36.6189 μM | SANGER | ||
| L-540 | Growth Inhibition Assay | IC50=37.2308 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=38.8846 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=39.9651 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=42.415 μM | SANGER | ||
| BC-3 | Growth Inhibition Assay | IC50=45.4896 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=45.5474 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=45.666 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=46.018 μM | SANGER | ||
| SKBR3 | Cytotoxicity assay | Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.002 μM. | 21080629 | ||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.003 μM. | 21080629 | ||
| CAL27 | Cytotoxicity assay | Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.007 μM. | 21080629 | ||
| 4T1 | Cytotoxicity assay | Cytotoxicity against mouse triple negative 4T1 cells, IC50 = 0.01037 μM. | 24890652 | ||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human triple negative MDA-MB-231 cells, IC50 = 0.02 μM. | 24890652 | ||
| BT474 | Antiproliferative assay | Antiproliferative activity against human BT474 cells overexpressing ErB2, IC50 = 0.025 μM. | 18653333 | ||
| HEK293 | Function assay | Inhibition of recombinant human C-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.02706 μM. | 28711703 | ||
| HEK293 | Function assay | Inhibition of recombinant human N-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.0271 μM. | 29421573 | ||
| HepG2 | Function assay | Inhibition of EGFR in human HepG2 cells, IC50 = 0.0271 μM. | 30096580 | ||
| MDA-MB-435 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-435 cells, IC50 = 0.0297 μM. | 24890652 | ||
| SK-BR-3 | Antiproliferative assay | Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay, IC50 = 0.04 μM. | 20143778 | ||
| A431 | Function assay | Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.052 μM. | 20346655 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human ER-positive MCF7 cells, IC50 = 0.0649 μM. | 24890652 | ||
| MDA-MB-468 | Cytotoxicity assay | Cytotoxicity against human triple negative MDA-MB-468 cells, IC50 = 0.0832 μM. | 24890652 | ||
| N87 | Function assay | Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA, IC50 = 0.1 μM. | 20346655 | ||
| MIAPaCa | Function assay | Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.14 μM. | 20817523 | ||
| MIAPaCa | Function assay | Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.433 μM. | 20817523 | ||
| A431 | Cytotoxicity assay | Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.97 μM. | 21080629 | ||
| SK-BR-3 | Antiproliferative assay | Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay, IC50 = 4.35 μM. | 21570843 | ||
| HeLa | Cytotoxicity assay | Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 5.9 μM. | 21080629 | ||
| HepG2 | Antiproliferative assay | Antiproliferative activity against human HepG2 cells after hrs by ATP content assay, IC50 = 6.27 μM. | 20143778 | ||
| HepG2 | Cytotoxicity assay | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability, TC50 = 6.27 μM. | 29049963 | ||
| HepG2 | Cytotoxicity assay | Cytotoxicity against human HepG2 cells, TC50 = 6.3 μM. | 30344906 | ||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 8.5 μM. | 21080629 | ||
| MDA-MB-468 | Antiproliferative assay | Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay, IC50 = 23.46 μM. | 21570843 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 42.36 μM. | 21570843 | ||
| NCI-N87 | Antitumor assay | Antitumor activity against human NCI-N87 cells xenografted in athymic mouse assessed as tumor growth inhibition at 20 mg/kg, po QD for 14 days measured after 19 days | 22101132 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS 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 | ||
| 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 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| NCI-H522 | Antitumor assay | Antitumor activity against human NCI-H522 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 100 mg/kg, ig administered once daily for 28 days relative to control | 28092860 | ||
| LLC | Antitumor assay | Antitumor activity against mouse LLC cells implanted in in C57BL/6 mouse assessed as tumor growth inhibition at 100 mg/kg, po qd for 14 days | 27187856 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Lapatinib，以 Lapatinib Ditosylate的形式使用，是一种有效的EGFR和ErbB2抑制剂，在无细胞试验中IC50分别为10.2和9.8 nM。Lapatinib 可诱导 ferroptosis 和细胞自噬。 | ||||||
|---|---|---|---|---|---|---|---|
| 特性 | Lapatinib 已经批准用于治疗HER-2阳性转移性乳腺癌。[2] | ||||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 除了ErbB-4例外, Lapatinib 作用于EGFR 和 ErbB-2比作用于其他测试的激酶，如c-Src, MEK和ERK选择性高300多倍。Lapatinib处理，抑制EGFR 和ErbB-2受体自磷酸化，这种作用存在剂量依赖性，作用于 BT474 和HN5 细胞时，IC50 分别为 0.17 和 0.08 μM。Lapatinib作用于EGFR-和ErbB-2-过量表达的肿瘤细胞，抑制EGFR 和ErbB-2自磷酸化，比作用于纯化酶的效力低10倍左右。Lapatinib 抑制 EGFR- 和ErbB-2过量表达的细胞生长，而OSI-774和 Iressa（都为EGFR选择性抑制剂）优先抑制 EGFR过量表达的细胞生长。Lapatinib作用于肿瘤细胞比作用于正常成纤维细胞效果高100倍左右。ErbB-2转染的乳腺上皮细胞HB4a c5.2,对 Lapatinib的反应敏感度比未转染的亲本对照细胞HB4a高40倍左右。使用不含Lapatinib 的培养基培养HN5 细胞群2周左右后，使用30 μM Lapatinib 短暂处理，完全抑制细胞生长。浓度>3.3 μM时抑制50%生长。浓度为0.37 μM时抑制20%生长。另一种EGFR过量表达的细胞A-431, 与HN5反应相似。Lapatinib在抑制 EGFR过量表达的细胞生长方面与 OSI-774 相似。[1] | |||
|---|---|---|---|---|
| 激酶实验 | 体外EGFR, ErbB-2,和 ErbB4激酶实验 | |||
| 从杆状病毒表达系统中纯化EGFR, ErbB-2, 和 ErbB4的细胞内激酶域。EGFR, ErbB-2, 和 ErbB-4 反应在96孔聚苯乙烯圆底板中进行，终体积为45 μL。反应混合物含50 mM 4-吗啉基丙磺酸(pH 7.5), 2 mM MnCl2,10 μM ATP, 1 μCi [γ-33 P] ATP/每次反应,50 μM Peptide A [生物素-(氨基酸)-EEEEYFELVAKKK-CONH2],1 mM 二硫苏糖醇, 及 1 μL 含连续稀释Lapatinib（初浓度为10 μM）的 DMSO。加入指定纯化的1型受体细胞内域开始反应。加入的酶量为1 pmol/每次反应 (20 nM)。在23oC反应10分钟，加入溶于水的 45 μL 0.5% 磷酸后，终止反应。最终反应混合物(75 μL) 转移到磷酸纤维素过滤板上。过滤实验板，使用200 μL 0.5% 磷酸冲洗三次。每孔中加入闪烁混合物(50 μL),使用Packard Topcount计数而量化实验结果。 | ||||
| 细胞实验 | 细胞系 | HFF , BT474, MCF-7, N87, CaLu-3, HN5, A-431, T47D, HB4a, 和 HB4a c5.2 | ||
| 浓度 | 0 到 100 nM | |||
| 孵育时间 | 3 天 | |||
| 方法 | 按以下密度接种细胞：HFF, 1.5×104 个细胞/cm2; BT474, MCF-7, N87, 和 CaLu-3, 3×104 个细胞/cm2; 及HN5, A-431, T47D, HB4a, 和 HB4a c5.2, 1×104 个细胞/cm2，使在实验期间细胞处于对数生长期。24 小时后,使用浓度范围为0 到 100 nM的Lapatinib处理细胞。在含5% FBS, 50 μg/mL gentamicin, 和 0.3% v/v DMSO的低糖DMEM培养基中处理HFF, BT474,HN5, 和 N87 细胞。在50% 高糖DMEM,和50%含5% FBS, 50 μg/mL gentamicin, 和 0.3% v/v DMSO的低糖DMEM中处理MCF-7细胞。在 50% RPMI,50%含 5% FBS, 50 μg/mL gentamicin, 和 0.3% v/v DMSO 的低糖DMEM中处理T47D, A-431, 和CaLu-3 细胞。在50% DMEM, 50% 含5% FBS, 2.5 μg/mL hydrocortisone, 2.5 μg/mL 胰岛素, 25 μg/mL hygromycin B, 50 μg/mL gentamicin, 和 0.3% v/v DMSO的RPMI 1640中处理HB4a 和 HB4a c5.2细胞。3天后, 使用亚甲基蓝染色测评相对细胞数。移除培养基，每孔加入溶解在 50% 乙醇和50% 水中的100 μL 0.5% w/v亚甲基蓝。浸泡在去离子水中洗涤实验板，然后在空气中烘干。每孔加入溶解在PBS的1% w/v n-lauroylsarcosine(100 μL), 然后实验板在室温下温育30分钟。使用Spectra酶标仪在620 nm处测定吸光值。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1 |
|
29799521 | |
| Immunofluorescence | LC3 Vimentin / E-cadherin |
|
26637440 | |
| Growth inhibition assay | Cell viability (OE19) Cell viability (A431 cells) |
|
25350844 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Lapatinib有效抑制BT474 和HN5 人类移植瘤生长。使用30和 100 mg/kg Lapatinib 口服给药携带肿瘤的小鼠，每天两次，抑制肿瘤生长，这种作用存在剂量依赖性。按100 mg/kg 剂量处理完全抑制肿瘤生长。按这种剂量处理，在处理21天期间，有<10%肿瘤损失。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 雌性CD-1裸鼠和雌性C.B-17 SCID 小鼠 |
| Dosages | 100 mg/kg | |
| Administration | 口服，每天两次 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00455039 | Withdrawn | Breast Cancer |
University of New Mexico |
July 31 2023 | Phase 1|Phase 2 |
| NCT04608409 | Active not recruiting | Ovarian Cancer |
Frederick R. Ueland M.D.|National Cancer Institute (NCI)|University of Kentucky |
March 17 2021 | Phase 1 |
| NCT03075995 | Unknown status | Breast Cancer |
Sun Yat-sen University |
April 12 2017 | Not Applicable |
| NCT02338245 | Completed | Metastatic Breast Cancer |
ASLAN Pharmaceuticals |
December 29 2014 | Phase 2 |
| NCT02294786 | Terminated | Cancer |
Novartis Pharmaceuticals|Novartis |
December 17 2014 | Phase 2 |
| NCT02158507 | Active not recruiting | Metastatic Triple Negative Breast Cancer |
University of Alabama at Birmingham|Breast Cancer Research Foundation of Alabama|GlaxoSmithKline|AbbVie |
September 2014 | Not Applicable |
化学信息&溶解度
| 分子量 | 581.06 | 分子式 | C29H26ClFN4O4S |
| CAS号 | 231277-92-2 | SDF | Download Lapatinib SDF |
| Smiles | CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (172.09 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : 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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* 必填项
常见问题及建议解决方法
问题 1:
If I want to use this compound(S2111, Lapatinib) in tumor-bearing mice via injection, how could I prepare the solution?
回答：
For I.P. administration, the compound solution should be clear solution. S2111 Lapatinib can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.
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