WZ8040 is a novel, irreversible mutant-selective EGFR kinase inhibitor that specifically inhibits phosphorylation of EGFRT790M.
WZ8040 shows to suppress the growth of EGFR T790M containing cell lines as well as inhibit phosphorylation of EGFR in the Non–Small-Cell Lung Cancer (NSCLC) cells. WZ8040 was identified from the screen that possessed up to a 300-fold lower IC50 against the PC9GR cells compared to clinical stage inhibitors such as HKI-272 [1].
References:
[1] Zhou W1, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4. doi: 10.1038/nature08622.