产品描述:
CO-1686 is an irreversible kinase inhibitor that specifically targets mutant forms of the epidermal growth factor receptor (EGFR) including T790M (Ki = 21.5 nM) with significantly reduced activity at the wild-type form of the receptor (Ki = 303.3 nM).{27821} CO-1686 has been shown to inhibit the proliferation of non-small cell lung cancer (NSCLC) cells expressing mutant EGFR with GI50 values ranging from 7-32 nM in vitro, inducing apoptosis.{27821} It also demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft and transgenic models dosed orally at 100 mg/kg/day.{27821}