AC480

AC480 is a dual inhibitor of EGFR and HER2 (IC50s = 22 and 32 nM, respectively). It is selective for EGFR and HER2 over HER4 (IC50 = 190 nM) and a panel of 21 additional kinases (IC50s = >2,500 nM for all). AC480 inhibits proliferation in a panel of EGFR and/or HER2 signaling-dependent cancer cells (IC50s = 0.24-0.94 μM). It reduces tumor growth in a Sal2 murine salivary gland tumor model, as well as GEO colon and KPL4 breast cancer mouse xenograft models in a dose-dependent manner. AC480 (100 mg/kg) reduces tumor cell motility, intravasation, and EGF-induced invasion in an MTLn3E metastatic mammary...