CGP 52411/CGP52411

 Home / Products / Inhibitors / EGFR inhibitor / CGP 52411/CGP52411
CGP 52411/CGP52411

CGP 52411/CGP52411

Cat.No.ABP000886 Chemical NameCGP 52411/CGP52411 CAS145915-58-8 MDL: MFCD00236442 MolFormulaC20H15N3O2 MolWeight329.358 Purity >99 %

Chemical Name : CGP 52411/CGP52411

CAS : 145915-58-8

Synonyms: DAPH


Storage:at -20℃ 2 years


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.


[1] Zhou W et al. Nature. 2009 Dec 24;462(7276):1070-4