Raf inhibitor 1

Raf inhibitor 1 is a potent Raf kinase inhibitor with K_is of 1 nM, 1 nM, and 0.3 nM for B-Raf^WT, B-Raf^V600E, and C-Raf, respectively. IC50 & Target: Ki: 1 nM (B-Raf^WT), 1 nM (B-Raf^V600E), 0.3 nM (C-Raf)^[1] In Vitro: Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC₅₀s of 0.31 and 0.72 μM, respectively. Raf inhibitor 1 (Compound 13) binds to and stabilizes B-Raf in a DFG-out, inactive conformation in which the ATP pocket is partially filled by Phe595 and Gly596 from the DFG motif. Raf inhibitor 1 (Compound 13) additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers^[1].