Description | A dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively); selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 µM) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively); induces ubiquitination and degradation of HER2 in SK-BR-3 cells at 10 and 30 µM; decreases levels of HER2 and ERα and increases levels of Hsp70 in MCF-7 cells at 10 µM; inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 µM); reduces tumor growth in an A431 mouse xenograft model at 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg |