Description
An inhibitor of mutant EGFR (IC50 = 0.01 µM for EGFRT790M/L858R); selective for EGFRT790M/L858R over PI3Kα (IC50 = >10 µM); cytotoxic to A549, H1975, H460, and MCF-7 cells (IC50s = 4.29, 0.52, 5.29, and 26.9 µM, respectively); reduces tumor growth in an ETS1-overexpressing doxorubicin-resistant K562 leukemia mouse xenograft model at 30 mg/kg in combination with doxorubicin