B-Raf inhibitor 1 dihydrochloride is a potentRafkinase inhibitor withK_is of 1 nM, 1 nM, and 0.3 nM for B-Raf^WT, B-Raf^V600E, andC-Raf, respectively.

B-Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC₅₀s of 0.31 and 0.72 μM, respectively. B-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. B-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].

551.86

C₂₆H₂₁Cl₃N₈

1191385-19-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.