RAF265, also known as CHIR-265, is a novel and orally available small molecule inhibitor of multiple intracellular kinases, including BRAFV600E, BRAF (wild-type), c-RAF, vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), colony-stimulating factor (CSF) 1R, RET, c-KIT, SRC and STE20, with half maximal inhibitory concentration IC50 ranging from less than 20 nmo/L to more than 100 nmol/L, in which it exhibits the highest potency for BRAFV600E and VEGFR2 with half maximal effective concentration EC50 of 0.14 μM and 0.19 μM respectively. RAF265 has been found to inhibit proliferation of melanoma and colorectal cancer cell lines with active BRAF mutations and time- and dose-dependently suppress tumor regression in BRAFV600E melanoma and colorectal cancer xenograft models.