Product Name: PLX-4032

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CAT#: A-1130


  Synonym:PLX-4032; RG7204, RO5185426, Vemurafenib

PLX-4032 Chemical Structure
PLX-4032 chemical structure


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

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Biological Activity

Vemurafenib (also known as PLX4032, RG7204 or RO5185426, marketed as Zelboraf) is an orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. Vemurafenib received FDA approval for the treatment of late-stage melanoma on August 17, 2011. 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. Approximately 90% of BRAF gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E); the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors, including melanoma, colorectal, thyroid and other cancers. Vemurafenib received FDA approval for the treatment of late-stage melanoma on August 17, 2011.

Technical Data

Formula:C23H18ClF2N3O3S
CAS#:1029872-54-5
M.Wt: 489.92
Purity:>99%
Storage Conditions :Room temperature, or -20ºC for 2 year.
PLX-4032 MSDS PLX-4032 CoA

Reference

1. Nature advance online publication 7 September 2010 | doi:10.1038/nature09454; Received 19 May 2010; Accepted 31 August 2010; Published online 7 September 2010
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma