Vemurafenib (PLX4032; RG7204; RO5185426)

Description: Vemurafenib (formerly PLX-4032; RG7204; RG-7204; RO5185426; RO-5185426; PLX4032; trade name: Zelboraf) is a potent and selective inhibitor of B-RafV600E mutated form with potential antineoplastic activity. It inhibits B-RafV600E with an IC50 of 31 nM in enzymatic assay. As an orally bioavailable, ATP-competitive and small-molecule inhibitor of BRAF(V600E) kinase, vemurafenib was approved by FDA in 2011 for the treatment of late-stage melanoma. Vemurafenib selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation.

References: Yang H, et al. Cancer Res, 2010, 70(13), 5518-5527.

Related CAS #: 918504-65-1; 918505-61-0 (analog);

Vemurafenib; RO5185426; RG7204; PLX 4032; RG 7204; RO 5185426; RG-7204; RO5185426; PLX4032; PLX-4032; trade name: Zelboraf

Chemical Name: N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2, 3-b]pyridine-3-carbonyl)-2, 4-difluorophenyl)propane-1-sulfonamide