Description | A RAF inhibitor (IC50s = 0.8, 0.8, and 0.6 nM for B-RAFV600E, wild-type B-RAF, and C-RAF in the DFG-out inactive conformation, respectively); selective for RAF over a panel of kinases, including LCK, KIT, Src, LYNA, LYNB, and PDGFR (IC50s = 49, 415, 485, 750, 715, and 1,220 nM, respectively); inhibits proliferation of human B-RAF-mutant melanoma cells at 1-10 nM; reduces tumor growth in multiple B-RAF-mutant melanoma and colorectal carcinoma mouse xenograft models at 25 mg/kg twice per day |