PLX-4720 (PLX4720) is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM.
PLX-4720 dispalys 10-fold selectivity over wild-type B-Raf, and remarkably selective against a diverse panel of 70 other kinases.
PLX-4720 inhibits ERK phosphorylation in COLO25 cells with IC50 of 14 nM.
PLX-4720 induces cell cycle arrest and apoptosis exclusively in B-Raf(V600E)-positive cells.
PLX-4720 inhibits tumor growth in B-Raf(V600E)-dependent tumor xenograft models; orally active.
