Description

RAF265 is an orally bioavailable anticancer chemotherapeutic compound that inhibits primarily WT B-Raf, mutant (V600E) B-Raf, and VEGFR2, but is also active against c-Raf, PDGFR, CSF-1R, RET, c-Kit, Src, and STE20. This compound is in clinical trials as a treatment for unresectable or metastatic melanoma. Inhibition of B-Raf by RAF265 attenuates downstream ERK and RET signaling, preventing tumor cell proliferation. Raf265-induced alterations in ERK signaling also decreases expression of c-fos and NFATc1, inhibiting in vitro differentiation of PBMCs to osteoclasts and inhibiting osteoclast resorptive capacity, therefore inhibiting osteoclastogenesis.