PLX-4720

PLX-4720 is a potent, orally available, ATP-competitive small molecule inhibitor that selectively targets the B-Raf V600E mutant kinase with an IC50 of 13 nM. It demonstrates approximately 10-fold selectivity for B-Raf V600E over wild-type B-Raf and also inhibits certain mutant forms of c-Raf-1. Mechanistically, PLX-4720 blocks ERK phosphorylation in tumor cell lines harboring the B-Raf V600E mutation, leading to cell cycle arrest and apoptosis specifically in these cells. Preclinical studies have shown significant antitumor activity in melanoma and thyroid cancer models. Developed by Plexxikon as a pre-clinical analog of vemurafenib, PLX-4720 did not advance to clinical trials[1][3][4][5][6][8].

Other names

PLX4720PLX-4720PLX 4720Raf Kinase Inhibitor VN-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide