950736-05-7

B-RAF IN 1 is an inhibitor of B-RAF (IC₅₀ = 24 nM) that also inhibits C-RAF (IC₅₀ = 25 nM). It is selective over 13 other kinases, including PKCα, IKKβ, and PI3Kα, at concentrations greater than 2 μM, but does inhibit p38α and CAMKII (IC₅₀s = 216 and 822 nM, respectively). B-RAF IN 1 binds to B-RAF in the inactive conformation based on co-crystallization with the wild-type enzyme. It inhibits proliferation of WM 266-4 and HT29 cells with IC₅₀ values of 920 and 780 nM, respectively.

N-[3-[3-[4-[(Dimethylamino)methyl]phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-3-(trifluoromethyl)benzamide is a potent and selective B-Raf inhibitor.