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Product Details:

  • CAS No: 918504-65-1
  • AHFC code: 10:00
  • Synonyms: BRAF(V600E) Kinase Inhibitor RO5185426
  • ATC Code: L01XE15
  • Chemical Formula: C23H18ClF2N3O3S
  • Molecular Weight: 489.922
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB08881
  • SMILES: CCCS(=O)(=O)NC1=C(F)C(C(=O)C2=CNC3=NC=C(C=C23)C2=CC=C(Cl)C=C2)=C(F)C=C1
  • InChl:
  • PubChem:
  • IUPAC: N-{3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl}propane-1-sulfonamide

Additional Details

Treatment of unresectable or metastatic melanoma in patients with the BRAF-V600 mutation.
Mode of Action:
Vemurafenib is an orally available inhibitor of mutated BRAF-serine-threonine kinase. It is especially potent against the BRAF V600E mutation. This mutation involves the substitution of glutamic acid for valine at codon 600. The BRAF oncogene, most of which have the V600E mutation, activates mitogen-activated kinase (MAPK) pathway which results in cell growth, proliferation, and metastasis. Vemurafenib blocks these downstream processes to inhibit tumour growth and eventually trigger apoptosis. Vemurafenib does not have antitumour effects against melanoma cell lines with the wild-type BRAF mutation.
Vemurafenib is metabolized by CYP3A4 and the metabolites make up 5% of the components in plasma. The parent compound makes up for the remaining 95%.
General Reference:
Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. Pubmed
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