RAF265 is a dual inhibitor of mutant B-RafV600E and vascular endothelial growth factor receptor 2 (EC50s = 0.14 and 0.19 μM, respectively, in cell-based assays). It can also inhibit wild-type B-Raf, platelet-derived growth factor receptor, colony-stimulating factor 1R, RET, c-KIT, SRC, and STE20 with IC50 values ranging from 20-100 nM. RAF265 can inhibit proliferation of melanoma and colorectal cancer cell lines with active BRAF mutations as well as suppress tumor growth in melanoma xenograft models bearing B-RafV600E mutations.
