Description
A potent and selective inhibitor of B-Raf V600E with IC50 of 13nM; dispalys 10-fold selectivity over wild-type B-Raf, and remarkably selective against a diverse panel of 70 other kinases; inhibits ERK phosphorylation in COLO25 cells with IC50 of 14nM; induces cell cycle arrest and apoptosis exclusively in B-Raf (V600E)-positive cells. In B-Raf (V600E)-dependent tumor xenograft models; orally active. Skin Cancer Preclinical