An inhibitor of mutant EGFR
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].
参考文献:
[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,?J?nne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature.?2009 Dec 24;462(7276):1070-4. doi: 10.1038/nature08622.
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