Description
A potent inhibitor of mutant EGFRs (IC50s = 0.076, 0.049, 0.002, and 1.6 µM for recombinant EGFRL858R, EGFRT790M, EGFRL858R/T790M, and wild-type EGFR, respectively); inhibits phosphorylation of EGFR in a concentration-dependent manner in H1975 cells; reduces proliferation of Ba/F3 cells expressing EGFRL858R/T790M and EGFRL858R/T790M/I941R from 0.01-10 µM; induces tumor regression and reduces EGFR signaling in mice bearing EGFRL858R/T790M, EGFRExon19del/T790M, and EGFRL858R/T790M/C797S tumors at 60 mg/kg/day with cetuximab