plx7904

Description: PLX7904 (also known as PB04) is a novel potent and selective paradox-breaker B-Raf inhibitor with IC50 of ca.5 nM against BRAFV600E in mutant RAS expressing cells. It inhibits the growth of two melanoma cell lines (A375 and COLO829) and human colorectal cancer cell line COLO205 that expressed BRAFV600E with IC50 values of 0.17 uM, 0.53 uM, and 0.16 uM, respectively. PLX7904 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. PLX7940 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.

References: Nature. 2015 Oct 22; 526(7574):583-6; Pigment Cell Melanoma Res. 2013 Jul; 26(4):509-17.