Vemurafenib

  • Chemical Properties
CAS No. 1029872-54-5 Cat. No. BCP43160
Name Vemurafenib
Synonyms PLX4032;PLX-4032;PLX 4032;
Formula C23H18ClF2N3O3S M. Wt 489.92
  • Biological Activity
Description Vemurafenib is an orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. 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.
Related Products 918504-65-1(Vemurafenib)
Pathways MAPK Pathway 
Targets Raf 

Structure

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