化学名称 : 4,5-二苯胺基酞酰亚胺
CAS : 145915-58-8
英文名称: CGP 52411/CGP52411
英文同义词: DAPH
溶解度:DMSO
储存条件:at -20℃ 2 years
生物活性
WZ8040 is an irreversiblely EGFR T790M inhibitor (IC50<10nM).
WZ8040 is an irreversiblely inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) which is detected in 50% of clinically resistant patients to gefitinib or erlotinib. WZ8040 has a basic chemical framework (covalent pyrimidine) which is different from that of other EGFR inhibitors. [1]
This agent is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wildtype EGFR, than quinazoline-based EGFR inhibitors (HKI-272 and CL-387,785) in vitro. [1]
WZ8040 has a 300-fold lower half-maximum inhibitory concentration (IC50<10nM) against the PC9GR(delE746_A750/T790M, gefitinib-resistant) cells compared with clinical-stage inhibitors such as HKI-272.
参考文献