CCT-196969

CCT-196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRafV600E and CRAF with IC₅₀s of 0.1, 0.04, and 0.01 μM, respectively. It is selective for RAFs, Src, LCK, and MAPKs in a panel of 63 kinases when used at a concentration of 1 μM. CCT-196969 inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells, but not B-RAF wild-type D35 cells, and inhibits growth of B-RAF mutant melanoma cells in a concentration-dependent manner.