Crizotinib
别名: PF-02341066 中文名称：
Crizotinib克唑替尼是一种有效的c-Met和ALK抑制剂，在细胞试验中IC50分别为11 nM 和 24 nM。它同时也是有效的ROS1抑制剂，其Ki值小于0.025 nM。Crizotinib可在多种肺癌细胞系中通过抑制STAT3通路来诱导自噬。
Crizotinib Chemical Structure
CAS: 877399-52-5
产品质控
批次：
纯度：
99.9%
99.9
常与Crizotinib一起在实验中被使用的化合物
与Crizotinib作为ALK阳性NSCLC一线治疗药物相比，Ceritinib可显着延长无进展生存期(PFS)。
Alectinib在ALK阳性NSCLC的初级治疗中比Crizotinib具有更佳的疗效和更低的毒性。
与接受Crizotinib治疗的患者相比，Brigatinib在ALK阳性NSCLC患者中表现出更长的无进展生存期。
Lorlatinib在ALK突变或ALK扩增神经母细胞瘤细胞系中是比Crizotinib更有效的ALK抑制剂。
Tucker ER, et al. Clin Cancer Res. 2023 Apr 3;29(7):1317-1331.
Crizotinib和Afatinib在MPM细胞中表现出抗增殖作用。
Crizotinib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 |
|---|---|---|---|---|---|
| Antitumor assay | BAF3 | 50 mg/kg | 2 weeks | Antitumor activity against mouse BAF3 cells expressing EML4-ALK fusion protein allografted in nude mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 2 weeks relative to vehicle-treated control | 24900831 |
| Function assay | H2228 | 0.5 uM | 3 hrs | Inhibition of ALK in human H2228 cells assessed as decrease in AKT phosphorylation at 0.5 uM after 3 hrs by Western blot method | 29091425 |
| Function assay | Ba/F3 | 0.1 to 1 uM | 72 hrs | Inhibition of human wild type EML4 fused ALK expressed in mouse Ba/F3 cells assessed as decrease in cell proliferation at 0.1 to 1 uM preincubated for 72 hrs followed by methyl-3H-thymidine incorporation measured after 8 hrs by filter scintillation counte | 29091425 |
| Function assay | Hs578T | 100 nM | 30 mins | Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human Hs578T cells assessed as decrease in MET phosphorylation at 100 nM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot m | 29701962 |
| Function assay | HCC1937 | 100 nM | 30 mins | Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human HCC1937 cells assessed as decrease in MET phosphorylation at 100 nM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot | 29701962 |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 1.148 μM. | 24819116 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 1.026 μM. | 24819116 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.843 μM. | 24819116 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.626 μM. | 24819116 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.605 μM. | 24819116 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.478 μM. | 24819116 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.165 μM. | 24819116 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA, IC50 = 0.08 μM. | 24819116 | |
| Antiproliferative assay | NIH/3T3 | 72 hrs | Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1/L1196M mutant after 72 hrs by MTT assay, IC50 = 0.606 μM. | 24785465 | |
| Antiproliferative assay | SUP-M2 | 72 hrs | Antiproliferative activity against human SUP-M2 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.174 μM. | 24785465 | |
| Antiproliferative assay | NIH/3T3 | 72 hrs | Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1 after 72 hrs by MTT assay, IC50 = 0.0954 μM. | 24785465 | |
| Cytotoxicity assay | BAF3 | 72 hrs | Cytotoxicity against mouse BAF3 cells assessed as growth inhibition after 72 hrs by [3H]-thymidine incorporation assay, IC50 = 0.98 μM. | 24468632 | |
| Function assay | BAF3 | 72 hrs | Inhibition of NPM/ALK L1196M mutant (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay, IC50 = 0.26 μM. | 24468632 | |
| Function assay | BAF3 | 72 hrs | Inhibition of NPM/ALK (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay, IC50 = 0.051 μM. | 24468632 | |
| Function assay | BAF3 | 72 hrs | Inhibition of NPM/ALK (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay, IC50 = 0.051 μM. | 24468632 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 3.039 μM. | 24432909 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 1.026 μM. | 24432909 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.843 μM. | 24432909 | |
| Function assay | NCI-H3122 | 72 hrs | Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK L1196M mutant after 72 hrs by CellTiter Glo assay, IC50 = 0.838 μM. | 24432909 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.626 μM. | 24432909 | |
| Function assay | NCI-H3122 | 72 hrs | Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK G1269A mutant after 72 hrs by CellTiter Glo assay, IC50 = 0.623 μM. | 24432909 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.605 μM. | 24432909 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.478 μM. | 24432909 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 0.165 μM. | 24432909 | |
| Function assay | NCI-H2228 | 72 hrs | Inhibition of ALK-fusion driven cell proliferation in human NCI-H2228 cells after 72 hrs by CellTiter Glo assay, IC50 = 0.118 μM. | 24432909 | |
| Function assay | NCI-H3122 | 72 hrs | Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells after 72 hrs by CellTiter Glo assay, IC50 = 0.108 μM. | 24432909 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA, IC50 = 0.08 μM. | 24432909 | |
| Function assay | KARPAS299 | 72 hrs | Inhibition of ALK-fusion driven cell proliferation in human KARPAS299 cells after 72 hrs by CellTiter Glo assay, IC50 = 0.062 μM. | 24432909 | |
| Antiproliferative assay | EBC1 | 72 hrs | Antiproliferative activity against human EBC1 cells expressing elevated levels of constitutively active c-Met after 72 hrs by SRB assay, IC50 = 0.053 μM. | 22863529 | |
| SNU5 | Growth Inhibition Assay | 72 h | IC50=0.016 μM | 23993328 | |
| SKOV3 | Growth Inhibition Assay | 72 h | IC50=12.85 μM | 23993328 | |
| SK-MEL-28 | Growth Inhibition Assay | 72 h | IC50=10.97 μM | 23993328 | |
| NCI-H661 | Growth Inhibition Assay | 72 h | IC50=11.47 μM | 23993328 | |
| NCI-H441 | Growth Inhibition Assay | 72 h | IC50=17.25 μM | 23993328 | |
| MKN45 | Growth Inhibition Assay | 72 h | IC50=0.013 μM | 23993328 | |
| MDA-MB-231 | Growth Inhibition Assay | 72 h | IC50=10.8 μM | 23993328 | |
| MCF7 | Growth Inhibition Assay | 72 h | IC50=9.58 μM | 23993328 | |
| HCT116 | Growth Inhibition Assay | 72 h | IC50=14.82 μM | 23993328 | |
| EBC1 | Growth Inhibition Assay | 72 h | IC50=0.023 μM | 23993328 | |
| KARPAS299 | Cytotoxic Assay | 2-3 d | IC50=0.0642 μM | 23742252 | |
| BAF3 | Function Assay | 2-3 d | Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay with IC50 of 3.479 μM | 23742252 | |
| BAF3 | Function Assay | 2-3 d | Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay with IC50 of 0.1508 μM | 23742252 | |
| BAF3 | Function Assay | 2-3 d | Inhibition of TEL-fused insulin receptor expressed with IC50 of 1.643 μM | 23742252 | |
| PAE | Function Assay | 1 h | Inhibition of TRKA assessed as growth factor-induced autophosphorylation with IC50 of 0.58 μM | 21812414 | |
| PAE | Function Assay | 1 h | Inhibition of TRKB assessed as growth factor-induced autophosphorylation with IC50 of 0.399 μM | 21812414 | |
| KARPAS299 | Kinase Assay | 1 h | Inhibition of ALK assessed as growth factor-induced autophosphorylation with IC50 of 0.02 μM | 21812414 | |
| Jurkat | Function Assay | 1 h | Inhibition of LCK assessed as growth factor-induced autophosphorylation with IC50 of 2.741 μM | 21812414 | |
| HEK293 | Function Assay | 1 h | Inhibition of IR assessed as growth factor-induced autophosphorylation with IC50 of 2.887 μM | 21812414 | |
| HEK293 | Function Assay | 1 h | Inhibition of AXL assessed as growth factor-induced autophosphorylation with IC50 of 0.294 μM | 21812414 | |
| BAF3-BCL | Function Assay | 1 h | Inhibition of ABL assessed as growth factor-induced autophosphorylation with IC50 of 1.159 μM | 21812414 | |
| A549 | Kinase Assay | 1 h | Inhibition of human recombinant c-MET kinase expressed assessed as inhibition of HGF-induced autophosphorylation with IC50 of 0.008 μM | 21812414 | |
| 3T3-E | Function Assay | 1 h | Inhibition of TIE2 assessed growth factor-induced autophosphorylation with IC50 of 0.448 μM | 21812414 | |
| 3T3 | Function Assay | 1 h | Inhibition of RON assessed as growth factor-induced autophosphorylation with IC50 of 0.08 μM | 21812414 | |
| BAF3 | Cytotoxic Assay | 48 h | Cytotoxicity against mouse BAF3 cells expressing Tel-ALK with IC50 of 0.19 μM | 21572589 | |
| BAF3 | Cytotoxic Assay | 48 h | Cytotoxicity against mouse BAF3 cells expressing EML4-ALK with IC50 of 0.28 μM | 21572589 | |
| BAF3 | Cytotoxic Assay | 48 h | Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 with IC50 of 2.2 μM | 21572589 | |
| BAF3 | Cytotoxic Assay | 48 h | Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 with IC50 of 0.62 μM | 21572589 | |
| Function assay | NIH-3T3 | 1 hr | Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA, IC50 = 3.039 μM. | 24819116 | |
| Function assay | MKN845 | 1 hr | Inhibition of c-Met phosphorylation in human MKN845 cells after 1 hr by western blotting, IC50 = 0.02 μM. | 24900750 | |
| Function assay | MKN845 | 90 mins | Inhibition of c-Met phosphorylation in human MKN845 cells after 90 mins by Sandwich-ELISA, IC50 = 0.02 μM. | 24900750 | |
| Function assay | karpas 299 | 90 mins | Inhibition of NPM-fused ALK phosphorylation (unknown origin) expressed in human karpas 299 cells after 90 mins by Sandwich-ELISA, IC50 = 0.11 μM. | 24900750 | |
| Cytotoxicity assay | NCI-H1993 | 48 hrs | Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay, IC50 = 0.061 μM. | 24900830 | |
| Cytotoxicity assay | NIH/3T3 | 48 hrs | Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay, IC50 = 0.364 μM. | 24900830 | |
| Cytotoxicity assay | A549 | 48 hrs | Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 4.084 μM. | 24900830 | |
| Cytotoxicity assay | NCI-H1975 | 48 hrs | Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay, IC50 = 7.551 μM. | 24900830 | |
| Antiproliferative assay | EBC1 | 72 hrs | Antiproliferative activity against cMET-amplified human EBC1 cells after 72 hrs, IC50 = 0.0069 μM. | 24900831 | |
| Antiproliferative assay | KARPAS299 | 72 hrs | Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs, IC50 = 0.2 μM. | 24900831 | |
| Antiproliferative assay | EBC1 | 72 hrs | Antiproliferative activity against human EBC1 cells after 72 hrs, IC50 = 0.021 μM. | 25537530 | |
| Antiproliferative assay | SNU5 | 72 hrs | Antiproliferative activity against human SNU5 cells after 72 hrs, IC50 = 0.0204 μM. | 26005523 | |
| Antiproliferative assay | EBC1 | 72 hrs | Antiproliferative activity against human EBC1 cells after 72 hrs, IC50 = 0.0218 μM. | 26005523 | |
| Antiproliferative assay | MKN45 | 72 hrs | Antiproliferative activity against human MKN45 cells after 72 hrs, IC50 = 0.0381 μM. | 26005523 | |
| Antiproliferative assay | BAF3/TPR-Met | 72 hrs | Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs, IC50 = 0.1274 μM. | 26005523 | |
| Antiproliferative assay | NCI-H3122 | 72 hrs | Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs, IC50 = 0.2612 μM. | 26476749 | |
| Antiproliferative assay | NCI-H3122 | 72 hrs | Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.032 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.056 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.056 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.065 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.081 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.144 μM. | 26568289 | |
| Antiproliferative assay | SMS-KCNR | 72 hrs | Antiproliferative activity against human SMS-KCNR cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.179 μM. | 26568289 | |
| Antiproliferative assay | Kelly | 72 hrs | Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.211 μM. | 26568289 | |
| Antiproliferative assay | LAN5 | 72 hrs | Antiproliferative activity against human LAN5 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.232 μM. | 26568289 | |
| Antiproliferative assay | DFCI76 | 72 hrs | Antiproliferative activity against human DFCI76 cells expressing EML4-ALK L1152R mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.233 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.328 μM. | 26568289 | |
| Antiproliferative assay | SK-N-SH | 72 hrs | Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.37 μM. | 26568289 | |
| Antiproliferative assay | CHLA20 | 72 hrs | Antiproliferative activity against human CHLA20 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.439 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.512 μM. | 26568289 | |
| Antiproliferative assay | SH-SY5Y | 72 hrs | Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.523 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.549 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.645 μM. | 26568289 | |
| Antiproliferative assay | SK-N-BE(2) | 72 hrs | Antiproliferative activity against human SK-N-BE(2) cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.71 μM. | 26568289 | |
| Function assay | Ba/F3 | 72 hrs | Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.857 μM. | 26568289 | |
| Cytotoxicity assay | BA/F3 | 72 hrs | Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.927 μM. | 26568289 | |
| Antiproliferative assay | LAN1 | 72 hrs | Antiproliferative activity against human LAN1 cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.346 μM. | 26568289 | |
| Antiproliferative assay | SK-N-FI | 72 hrs | Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.469 μM. | 26568289 | |
| Antiproliferative assay | SK-N-AS | 72 hrs | Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.473 μM. | 26568289 | |
| Antiproliferative assay | DFCI114 | 72 hrs | Antiproliferative activity against human DFCI114 cells expressing EML4-ALK G1269A mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.615 μM. | 26568289 | |
| Antiproliferative assay | EBC1 | 72 hrs | Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay, IC50 = 0.019 μM. | 26698536 | |
| Cytotoxicity assay | EBC1 | 72 hrs | Cytotoxicity against human EBC1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50 = 0.044 μM. | 27017548 | |
| Antiproliferative assay | KARPAS299 | 72 hrs | Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.103 μM. | 27131066 | |
| Antiproliferative assay | SUP-M2 | 72 hrs | Antiproliferative activity against human SUP-M2 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.112 μM. | 27131066 | |
| Antiproliferative assay | SU-DHL1 | 72 hrs | Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.136 μM. | 27131066 | |
| Antiproliferative assay | NCI-H3122 | 72 hrs | Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.21 μM. | 27131066 | |
| Function assay | NCI-H3122 | 72 hrs | Inhibition of ALK expressed in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB/CCK-8 assay, IC50 = 0.261 μM. | 27131066 | |
| Antiproliferative assay | NIH/3T3 | 72 hrs | Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay, IC50 = 0.283 μM. | 27131066 | |
| Antiproliferative assay | NIH/3T3 | 72 hrs | Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay, IC50 = 1.16 μM. | 27131066 | |
| Antiproliferative assay | ALK-positive KARPAS299 | 72 hrs | Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay, IC50 = 0.365 μM. | 27144831 | |
| Antiproliferative assay | ALK-negative U937 | 72 hrs | Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay, IC50 = 2.286 μM. | 27144831 | |
| Cytotoxicity assay | HepG2 | 72 hrs | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 3.7 μM. | 27396929 | |
| Cytotoxicity assay | MIAPaCa2 | 72 hrs | Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 7.16 μM. | 27396929 | |
| Cytotoxicity assay | HCC827 | 72 hrs | Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 7.25 μM. | 27396929 | |
| Cytotoxicity assay | KARPAS299 | 72 hrs | Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.068 μM. | 27474925 | |
| Cytotoxicity assay | HCC78 | 72 hrs | Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.34 μM. | 27474925 | |
| Antiproliferative assay | SU-DHL1 | 72 hrs | Antiproliferative activity against ALK constitutively activated human SU-DHL1 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.0923 μM. | 27769623 | |
| Antiproliferative assay | NCI-H3122 | 72 hrs | Antiproliferative activity against ALK constitutively activated human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.1009 μM. | 27769623 | |
| Antiproliferative assay | KARPAS299 | 72 hrs | Antiproliferative activity against ALK constitutively activated human KARPAS299 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.1049 μM. | 27769623 | |
| Cytotoxicity assay | EBC1 | 72 hrs | Cytotoxicity against human EBC1 cells assessed as decrease in cell viability after 72 hrs by Cell Titer-Glo assay, Activity = 0.013 μM. | 28755635 | |
| Cytotoxicity assay | MKN45 | 72 hrs | Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 72 hrs by Cell Titer-Glo assay, Activity = 0.022 μM. | 28755635 | |
| Cytotoxicity assay | PC3 | 72 hrs | Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 72 hrs by Cell Titer-Glo assay, Activity = 2.244 μM. | 28755635 | |
| Function assay | BAF3 | 72 hrs | Inhibition of EML4-fused ALK (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM. | 28850922 | |
| Function assay | BAF3 | 72 hrs | Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM. | 28850922 | |
| Function assay | BAF3 | 72 hrs | Inhibition of TEL-fused ALK (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM. | 28850922 | |
| Antiproliferative assay | NCI-H3122 | 72 hrs | Antiproliferative activity against human NCI-H3122 cells harboring EML4-fused ALK varian1 after 72 hrs by CellTiter-Glo assay, GI50 = 0.037 μM. | 28850922 | |
| Antiproliferative assay | NCI-H2228 | 72 hrs | Antiproliferative activity against human NCI-H2228 cells harboring EML4-fused ALK varian3 after 72 hrs by CellTiter-Glo assay, GI50 = 0.073 μM. | 28850922 | |
| Function assay | BAF3 | 72 hrs | Inhibition of TEL-fused ALK C1156Y mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.15 μM. | 28850922 | |
| Function assay | BAF3 | 72 hrs | Inhibition of full length ALK F1174L mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.32 μM. | 28850922 | |
| Function assay | BAF3 | 72 hrs | Inhibition of TEL-fused ALK G1202R mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.43 μM. | 28850922 | |
| Antiproliferative assay | CHL | 72 hrs | Antiproliferative activity against CHL cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.45 μM. | 28850922 | |
| Function assay | BAF3 | 72 hrs | Inhibition of TEL-fused ALK L1196M mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.59 μM. | 28850922 | |
| Antiproliferative assay | BAF3 | 72 hrs | Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 1.1 μM. | 28850922 | |
| Antiproliferative assay | CHO | 72 hrs | Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay, GI50 = 3.2 μM. | 28850922 | |
| Antiproliferative assay | NCI-H2228 | 72 hrs | Antiproliferative activity against human NCI-H2228 cells after 72 hrs by MTT assay, IC50 = 2.5 μM. | 29091425 | |
| Antiproliferative assay | H2228/CR | 72 hrs | Antiproliferative activity against human H2228/CR cells after 72 hrs by MTT assay, IC50 = 10 μM. | 29091425 | |
| Antiproliferative assay | KARPAS299 | 72 hrs | Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.087 μM. | 29174809 | |
| Antiproliferative assay | HCC78 | 72 hrs | Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.17 μM. | 29174809 | |
| Antiproliferative assay | NCI-H2228 | 72 hrs | Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.24 μM. | 29174809 | |
| Antiproliferative assay | NCI-H3122 | 48 hrs | Antiproliferative activity against human NCI-H3122 cells after 48 hrs by MTT assay, IC50 = 0.8 μM. | 29174814 | |
| Antiproliferative assay | HCC78 | 48 hrs | Antiproliferative activity against human HCC78 cells after 48 hrs by MTT assay, IC50 = 2 μM. | 29174814 | |
| Antiproliferative assay | EBC1 | 72 hrs | Antiproliferative activity against human EBC1 cells after 72 hrs by Alamarblue assay, IC50 = 0.013 μM. | 29202410 | |
| Antiproliferative assay | MKN45 | 72 hrs | Antiproliferative activity against human MKN45 cells after 72 hrs by Alamarblue assay, IC50 = 0.022 μM. | 29202410 | |
| Antiproliferative assay | MCF7 | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by Alamarblue assay relative to control, IC50 = 0.045 μM. | 29202410 | |
| Antiproliferative assay | A549 | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by Alamarblue assay relative to control, IC50 = 0.1343 μM. | 29202410 | |
| Antiproliferative assay | HCT116 | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by Alamarblue assay relative to control, IC50 = 0.2536 μM. | 29202410 | |
| Antiproliferative assay | SGC7901 | 72 hrs | Antiproliferative activity against human SGC7901 cells after 72 hrs by Alamarblue assay relative to control, IC50 = 0.3213 μM. | 29202410 | |
| Antiproliferative assay | NCI-H460 | 72 hrs | Antiproliferative activity against human NCI-H460 cells after 72 hrs by Alamarblue assay, IC50 = 2.244 μM. | 29202410 | |
| Antiproliferative assay | COLO205 | 72 hrs | Antiproliferative activity against human COLO205 cells after 72 hrs by Alamarblue assay, IC50 = 2.449 μM. | 29202410 | |
| Antiproliferative assay | PC3 | 72 hrs | Antiproliferative activity against human PC3 cells after 72 hrs by Alamarblue assay, IC50 = 9.787 μM. | 29202410 | |
| Antiproliferative assay | BAF3 | 72 hrs | Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay, IC50 = 0.0486 μM. | 29288940 | |
| Antiproliferative assay | BAF3 | 72 hrs | Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.0575 μM. | 29288940 | |
| Antiproliferative assay | SU-DHL1 | 72 hrs | Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.155 μM. | 29288940 | |
| Antiproliferative assay | KARPAS299 | 72 hrs | Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.176 μM. | 29288940 | |
| Antiproliferative assay | NCI-H3122 | 72 hrs | Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.303 μM. | 29288940 | |
| Antiproliferative assay | BAF3 | 72 hrs | Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.34 μM. | 29288940 | |
| Antiproliferative assay | BAF3 | 72 hrs | Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.564 μM. | 29288940 | |
| Antiproliferative assay | BAF3 | 72 hrs | Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.594 μM. | 29288940 | |
| Antiproliferative assay | BAF3 | 72 hrs | Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.644 μM. | 29288940 | |
| Antiproliferative assay | HCC78 | 72 hrs | Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay, IC50 = 0.889 μM. | 29288940 | |
| Antiproliferative assay | EBC1 | 72 hrs | Antiproliferative activity against human EBC1 cells after 72 hrs by Cell Titer-Glo assay, IC50 = 0.039 μM. | 29602036 | |
| Antiproliferative assay | NCI-H2228 | 72 hrs | Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.087 μM. | 30223120 | |
| Antiproliferative assay | HCC78 | 72 hrs | Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.17 μM. | 30223120 | |
| Antiproliferative assay | KARPAS299 | 72 hrs | Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.24 μM. | 30223120 | |
| SMS-KCN | Cytotoxic Assay | Cytotoxicity against human SMS-KCN cells expressing ALK R1275Q mutant with IC50 of 0.91 μM | 21572589 | ||
| SH-SY5Y | Cytotoxic Assay | Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant with IC50 of 0.53 μM | 21572589 | ||
| Kelly | Cytotoxic Assay | Cytotoxicity against human Kelly cells expressing ALK F1174L mutant with IC50 of 0.42 μM | 21572589 | ||
| SU-DHL1 | Cytotoxic Assay | Cytotoxicity against human SU-DHL1 cells expressing ALK coexpressing NPM with IC50 of 0.01 μM | 21572589 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.08 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.08 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK F1174L mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.165 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK F1174L mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.165 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK C1156Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.478 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK C1156Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.478 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK G1269A mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.605 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK G1269A mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.605 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK S1206Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.626 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK S1206Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.626 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK L1196M mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.843 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK L1196M mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.843 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK L1152R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 1.026 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK L1152R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 1.026 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK G1202R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 1.148 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK G1202R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 1.148 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK 1151Tins mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 3.039 μM. | 28431340 | ||
| Function assay | NIH/3T3 | Inhibition of wild type EML4/ALK 1151Tins mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 3.039 μM. | 28431340 | ||
| qHTS assay | TC32 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| qHTS assay | A673 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| qHTS assay | Saos-2 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| qHTS assay | RD | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| qHTS assay | SK-N-SH | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| qHTS assay | BT-12 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| qHTS assay | MG 63 (6-TG R) | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| qHTS assay | NB1643 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| qHTS assay | OHS-50 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| qHTS assay | LAN-5 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| qHTS assay | NB-EBc1 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | ||
| qHTS assay | SK-N-SH | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| qHTS assay | Rh41 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| qHTS assay | A673 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| qHTS assay | Rh30 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| qHTS assay | BT-37 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| qHTS assay | MG 63 (6-TG R) | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| qHTS assay | Rh30 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| qHTS assay | OHS-50 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| qHTS assay | SJ-GBM2 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| qHTS assay | SK-N-MC | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| qHTS assay | NB-EBc1 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| qHTS assay | LAN-5 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| qHTS assay | Rh18 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| qHTS assay | NB1643 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| qHTS assay | SK-N-MC | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| qHTS assay | TC32 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| qHTS assay | Rh18 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| qHTS assay | Saos-2 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| NB1 | Growth Inhibition Assay | IC50=91.98 nM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=105.75 nM | SANGER | ||
| SR | Growth Inhibition Assay | IC50=126.31 nM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=204.24 nM | SANGER | ||
| SU-DHL-1 | Growth Inhibition Assay | IC50=336.82 nM | SANGER | ||
| SCC-3 | Growth Inhibition Assay | IC50=356.76 nM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=369.9 nM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=596.48 nM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=601.34 nM | SANGER | ||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=682.57 nM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=706.9 nM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=749.75 nM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=857.66 nM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=1.05997 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=1.38282 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=1.40861 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=1.72269 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=1.76867 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=1.95575 μM | SANGER | ||
| CMK | Growth Inhibition Assay | IC50=1.96159 μM | SANGER | ||
| ST486 | Growth Inhibition Assay | IC50=2.43073 μM | SANGER | ||
| CI-1 | Growth Inhibition Assay | IC50=2.49659 μM | SANGER | ||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=2.70122 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=3.18207 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=3.21225 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=4.2393 μM | SANGER | ||
| GDM-1 | Growth Inhibition Assay | IC50=4.24617 μM | SANGER | ||
| BC-1 | Growth Inhibition Assay | IC50=4.49277 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=4.83524 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=5.33874 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=5.82151 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=6.08473 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=6.37773 μM | SANGER | ||
| NALM-6 | Growth Inhibition Assay | IC50=6.68387 μM | SANGER | ||
| EB-3 | Growth Inhibition Assay | IC50=7.07233 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=9.24329 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=9.59842 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=9.69653 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=9.74642 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=10.0567 μM | SANGER | ||
| RPMI-8402 | Growth Inhibition Assay | IC50=10.116 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=10.2991 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=10.4425 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=10.4844 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=10.5043 μM | SANGER | ||
| MFH-ino | Growth Inhibition Assay | IC50=10.8303 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=11.597 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=12.0436 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=12.1705 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=12.2041 μM | SANGER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=12.4872 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=12.7966 μM | SANGER | ||
| HCC1599 | Growth Inhibition Assay | IC50=12.9069 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=12.9586 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=13.2925 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=13.7989 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=14.0324 μM | SANGER | ||
| OPM-2 | Growth Inhibition Assay | IC50=14.4085 μM | SANGER | ||
| KARPAS-422 | Growth Inhibition Assay | IC50=14.5126 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=14.8915 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=15.7716 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=15.8631 μM | SANGER | ||
| LC-2 | Growth Inhibition Assay | IC50=16.1506 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=16.254 μM | SANGER | ||
| RL95-2 | Growth Inhibition Assay | IC50=16.3978 μM | SANGER | ||
| KNS-42 | Growth Inhibition Assay | IC50=16.7274 μM | SANGER | ||
| RPMI-6666 | Growth Inhibition Assay | IC50=16.9211 μM | SANGER | ||
| SIG-M5 | Growth Inhibition Assay | IC50=17.1903 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=17.7451 μM | SANGER | ||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=17.9312 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=18.7557 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=19.3059 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=20.2132 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=20.5221 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=20.9099 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=21.7221 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=21.7915 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=22.6564 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=22.8671 μM | SANGER | ||
| MRK-nu-1 | Growth Inhibition Assay | IC50=22.9074 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=23.76 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=24.003 μM | SANGER | ||
| NCI-H1963 | Growth Inhibition Assay | IC50=24.0782 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=24.8772 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=25.0723 μM | SANGER | ||
| LP-1 | Growth Inhibition Assay | IC50=25.6551 μM | SANGER | ||
| NCI-H748 | Growth Inhibition Assay | IC50=26.5137 μM | SANGER | ||
| PF-382 | Growth Inhibition Assay | IC50=27.2223 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=27.3732 μM | SANGER | ||
| L-540 | Growth Inhibition Assay | IC50=27.6459 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=27.7519 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=28.1807 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=30.3976 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=30.6899 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=30.8566 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=31.5893 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=33.9431 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=34.1756 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=34.5184 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=34.8535 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=35.0469 μM | SANGER | ||
| TE-15 | Growth Inhibition Assay | IC50=35.2238 μM | SANGER | ||
| LC4-1 | Growth Inhibition Assay | IC50=35.3847 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=36.1369 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=38.7347 μM | SANGER | ||
| SK-MM-2 | Growth Inhibition Assay | IC50=40.1146 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=41.0563 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=42.4883 μM | SANGER | ||
| CPC-N | Growth Inhibition Assay | IC50=42.9971 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=44.4153 μM | SANGER | ||
| Daudi | Growth Inhibition Assay | IC50=45.0827 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=45.0853 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=46.726 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=48.1933 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=48.3542 μM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=48.8476 μM | SANGER | ||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=49.2143 μM | SANGER | ||
| CESS | Growth Inhibition Assay | IC50=49.5088 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=49.9736 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Crizotinib克唑替尼是一种有效的c-Met和ALK抑制剂，在细胞试验中IC50分别为11 nM 和 24 nM。它同时也是有效的ROS1抑制剂，其Ki值小于0.025 nM。Crizotinib可在多种肺癌细胞系中通过抑制STAT3通路来诱导自噬。 | ||||||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | PF-2341066作用于mIMCD3小鼠和MDCK犬上皮细胞，作用于c-Met磷酸化作用时具有相似效果，IC50分别为5 nM 和20 nM。PF-2341066作用于表达c-Met ATP-结合位点突变型V1092I 或H1094R或 P-环突变 M1250T 的NIH3T3 细胞，具有相似的活性，且活力增高，IC50分别为19 nM,2 nM 和15 nM,而作用于表达野生型受体的NIH3T3 细胞时，IC50为13 nM。[1] 相反, 观察到PF-2341066作用于表达c-Met活化环突变型Y1230C 和Y1235D的细胞时，与作用于野生型受体相比，效果发生显著改变，IC50分别为127 nM 和92 nM。PF-2341066 作用于分别表达内源性c-Met 突变体R988C和 T1010I 的NCI-H69 和HOP92 细胞，也有效抑制c-Met 磷酸化, IC50分别为13 nM 和16 nM。与作用于c-Met相比，PF-2341066作用于VEGFR2 和PDGFRβ RTKs, 选择性高1000多倍，作用于IRK和Lck选择性高250多倍，作用于Tie2, TrkA,和TrkB选择性高40到60倍。PF-2341066 作用于RON和 Axl RTKs时选择性为20到30倍。相反，PF-2341066 作用于表达ALK RTK 的核磷蛋白 (NPM)- 间变性淋巴瘤激酶(ALK) 致癌融合突变体和 KARPAS299人间变性大细胞淋巴瘤(ALCL)细胞系时具有相近的IC50值，为24 nM。PF-2341066抑制c-Met依赖的癌细胞的肿瘤表现型，和内皮细胞的血管生成表现型。PF-2341066抑制人GTL-16胃癌细胞生长，IC50为9.7 nM。PF-2341066诱导 GTL-16细胞凋亡，IC50 为8.4 nM。PF-2341066 抑制HGF刺激的人NCI-H441肺癌细胞迁移和入侵，IC50分别为11 nM 和6.1 nM。PF-2341066抑制 MDCK细胞散射，IC50为16 nM。PF-2341066 抑制HGF-刺激的c-Met磷酸化,细胞存活，和Matrigel入侵，IC50分别为11 nM, 14 nM和35 nM。此外, PF-2341066抑制纤维蛋白胶中的血清刺激的 HMVEC分支小管形成 (形成血管)。[1] PF-2341066 作用于Karpas299 或SU-DHL-1 ALCL细胞，也有效抑制 NPM-ALK磷酸化，IC50 为24 nM。PF-2341066 有效抑制细胞增殖，伴随着使细胞周期停在G(1)-S期，且诱导 ALK阳性的 ALCL 细胞凋亡，IC50为30 nM, 但是作用于ALK阴性的淋巴瘤细胞则无效果。 [2] 此外, PF-2341066 抑制骨肉瘤的一些活动行为，及其肿瘤生长 (例如,增殖和存活)和转移 (例如，入侵和形成克隆)。[3] |
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|---|---|---|---|---|
| 激酶实验 | 生化激酶实验 | |||
| 使用连续耦合的分光光度测定c-Met催化活性，通过分析NADH消耗率而测定c-Met诱导的ADP产量，这种作用具有时间依赖性。在 340 nm处使用分光光度法在指定时间点测定吸光值的降低而计算NADH的消耗量。为了测定Ki值, 在含实验试剂的实验孔中加入不同浓度PF-2341066，然后在37oC下温育10分钟。加入c-Met酶开始进行实验反应。 | ||||
| 细胞实验 | 细胞系 | GTL-16胃癌细胞和T47D乳腺癌细胞 | ||
| 浓度 | 0 nM-256 nM | |||
| 孵育时间 | 1小时 | |||
| 方法 | GTL-16胃癌细胞和T47D乳腺癌细胞接种在96孔板上，孔中含培养基，培养基中含10% 胎牛血清(FBS)，然后转移到无血清培养基中[含0.04%牛血清蛋白(BSA)]，处理 24小时。 在调查配体依赖的RTK 磷酸化实验中，加入相应的生长因子，处理20分钟。细胞和 PF-2341066和/或适当配体在指定时间温育1小时，然后使用含 1 mmol/L Na3VO4的HBSS冲洗细胞一次,然后从细胞中获得蛋白裂解物。随后,通过夹心酶联免疫吸附试验法使用特定的捕获抗体在96孔板上测定选定蛋白激酶的磷酸化，使用特点检测抗体测定磷酸化的酪氨酸残基。抗体包被的实验板(a) 在蛋白裂解物存在时，在4oC下过夜;(b)在溶于PBS的1% Tween-20 中冲洗7次;(c)在辣根过氧化物酶标记的抗总磷酸（PY-20）抗体（1:500）中温育20分钟;(d) 再次冲洗7次;(e)在3,3′,5,5′-四甲基联苯胺过氧化物酶底物中温育，开始显示反应，加入0.09 N H2SO4终止反应; (f)在450 nm 处使用分光光度计测定吸光度。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pALK / pAKT / pERK / pS6 pROS1 / ROS1 pSTAT3 / STAT3 PARP / cleaved caspase-3 / Bax / Bcl-2 p-c-Met / c-Met p-mTOR |
|
24675041 | |
| Immunofluorescence | LC3 / lysosome SRC / Met α-tubulin cytochrome c p-ALK |
|
26384345 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | PF-2341066每天按50 mg/kg和75 mg/kg剂量处理GTL-16 模型, 引起大肿瘤 (体积大于600 mm3) 明显衰退，且按43天处理日程处理后，平均肿瘤体积降低60%。在另一项研究中, PF-2341066处理3个月以上，完全抑制GTL-16肿瘤生长，PF-2341066每天按50 mg/kg剂量处理小鼠，3个月后，只有1/12小鼠的肿瘤生长得到提高。PF-2341066每天按50 mg/kg剂量处理NCI-H441 NSCLC 模型处理周期为38天，观察到平均肿瘤体积降低43%。PF-2341066 每天按50 mg/kg剂量作用于 Caki-1 RCC模型，处理周期为33天，观察到平均肿瘤体积降低53%，且每种肿瘤体积降低至少30%。PF-2341066每天按 50 mg/kg剂量作用于 U87MG 恶性胶质瘤或PC-3前列腺癌移植瘤模型,几乎完全抑制肿瘤生长，在实验最后一天，抑制分别达97% 或84%。相反, PF-2341066每天按50 mg/kg剂量口服给药处理 MDA-MB-231 乳腺癌模型,或 DLD-1 结肠癌模型，不会显著抑制肿瘤生长。PF-2341066每天按12.5 mg/kg, 25 mg/kg, 和50 mg/kg剂量作用于 GTL-16 肿瘤，观察到CD31阳性内皮细胞显著降低，这种作用存在剂量依赖性，说明 MVD 受抑制，且具有相关的抗癌高效性，这种作用也存在剂量依赖性。PF-2341066 作用于GTL-16 和 U87MG 模型，显著降低人VEGFA 和IL-8血浆水平，这种作用存在剂量依赖性。PF-2341066口服处理GTL-16 肿瘤，观察到磷酸化的c-Met, Akt, Erk, PLCλ1,和 STAT5水平显著受抑制。[1]PF-2341066 每天按100 mg/kg剂量口服处理携带Karpas299 ALCL 移植瘤的SCID Beige 小鼠，具有抗癌高效性，这种作用存在剂量依赖性，处理15天，所有肿瘤完全衰退。此外, PF-2341066抑制关键NPM-ALK信号调节器, 包括磷脂酶C-γ, 信号转导器，及转录因子3, 细胞外信号调节激酶, 和Akt的激活剂，这些与 NPM-ALK 磷酸化和功能受抑制相关。[2] PF-2341066 抑制骨肉瘤的一些活动行为，及其肿瘤生长(例如, 增殖和存活)和转移 (例如，入侵和形成克隆)。PF-2341066口服饲喂裸鼠，抑制生长和相关的骨肉瘤裸鼠移植瘤的骨基质的形成。[3] PF-2341066 按50 mg/kg 剂量处理 c-MET-扩增的GTL-16移植瘤，引起肿瘤衰退，这与18F-FDG 摄取的缓慢降低相关，且降低葡糖糖转运蛋白 1, GLUT-1的表达。[4] |
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|---|---|---|
| 动物实验 | Animal Models | 携带NCI-H441,或DLD-1,或MDA-MB-231的雌性和雄性nu/nu小鼠 |
| Dosages | 12.5 mg/kg/day, 25 mg/kg/day, 和50 mg/kg/day | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06062810 | Not yet recruiting | Non-Small Cell Lung Cancer |
Han Xu M.D. Ph.D. FAPCR Sponsor-Investigator IRB Chair|Medicine Invention Design Inc |
March 28 2024 | Phase 2|Phase 3 |
| NCT04148066 | Completed | Carcinoma Non-Small-Cell Lung |
The Netherlands Cancer Institute|Roche Pharma AG |
July 17 2019 | Not Applicable |
| NCT03947385 | Recruiting | Metastatic Uveal Melanoma|Cutaneous Melanoma|Colorectal Cancer|Other Solid Tumors |
IDEAYA Biosciences |
June 28 2019 | Phase 1|Phase 2 |
| NCT03672643 | Terminated | ALK or ROS1-positive NSCLC |
Pfizer |
January 28 2019 | Phase 4 |
| NCT03439215 | Unknown status | Carcinoma Non-Small-Cell Lung |
Fondazione Ricerca Traslazionale|Clinical research technology Srl |
June 13 2017 | Phase 2 |
化学信息&溶解度
| 分子量 | 450.34 | 分子式 | C21H22Cl2FN5O |
| CAS号 | 877399-52-5 | SDF | Download Crizotinib SDF |
| Smiles | CC(C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 25 mg/mL ( (55.51 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 |
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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:
Could you tell me whether this product represents the pure R-form of crizotinib, or is the the racemic Crizotinib, so a mixture of the S- and the R-form?
回答：
Our S1068 Crizotinib is R enantiomer(except batch 05 and 06, they are racemate), and S7505 is S enantiomer.
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