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CAS No.: 1213269-23-8
Synonyms: WZ4002
WZ4002 is an irreversible inhibitor of mutant EGFR (L858R) and EGFR (T790M) with IC50 of 2 nM and 8 nM respectively.
生物活性
靶点 | EGFR (L858R) IC50:2nM | EGFR (T790M) IC50:8nM |
实验方案
技术信息
CAS号 | 1213269-23-8 | 储存条件 |
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分子式 | C25H27ClN6O3 | 运输 | 蓝冰 | |||||||||||
分子量 | 494.97 | 别名 | WZ4002 | |||||||||||
溶解度 |
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动物实验配方 |
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Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
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human 16HBE cells | - | Proliferation assay | 72 h | Antiproliferative activity against human 16HBE cells expressing wild type EGFR after 72 hrs by MTT assay, IC50=0.811 μM | 23792318 |
human 16HBE14o- cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human 16HBE14o- cells harboring wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay, IC50=1.355 μM | 23668441 |
human A431 cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human A431 cells overexpressing wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay, IC50=1.108 μM | 23668441 |
human A549 cells | - | Proliferation assay | 72 h | Antiproliferative activity against k-RAS dependent human A549 cells overexpressing WT EGFR after 72 hrs by MTT assay, IC50=2.102 μM | 24607591 |
human BEAS2B cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human BEAS2B cells harboring wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay, IC50=1.811 μM | 23668441 |
human HCC827 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human HCC827 cells harboring EGFR del E746-A750 mutant after 72 hrs by MTS assay, IC50=7 nM | 22339342 |
human HL7702 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human HL7702 cells expressing wilt type EGFR after 72 hrs by MTS assay, IC50=2.73 μM | 22339342 |
human LoVo cells | - | Function assay | 2 h | Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay, IC50=1.18 μM | 23930994 |
human PC9 cells | - | Proliferation assay | - | Antiproliferative activity against growth-resistant human PC9 cells expressing EGFR E746_A750/T790M mutant, EC50=14 nM | 21208802 |
mouse BA/F3 cells | - | Proliferation assay | - | Antiproliferative activity against mouse BA/F3 cells transfected with EGFR E746_A750_del/T790M mutant, EC50=2 nM | 21208802 |
NCI-H1975 cells | - | Function assay | 2 h | Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay, IC50=0.023 μM | 23930994 |
Sf9 cells | - | Function assay | 60 mins | Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay, IC50=1 nM | 26275028 |
靶点 | Description | IC50 |
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EGFR (L858R) | IC50:2nM | |
EGFR (T790M) | IC50:8nM |
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