Vemurafenib, also known as PLX4032, RG7204 or RO5185426, 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.
Chemical Formula: C23H18ClF2N3O3S
Exact Mass: 489.07255
Molecular Weight: 489.92
Elemental Analysis: C, 56.39; H, 3.70; Cl, 7.24; F, 7.76; N, 8.58; O, 9.80; S, 6.54
RO 5185426 RO5185426 Vemurafenib
Brand name: Zelboraf
InChi Code: InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)
Appearance: White to off-white crystalline solid
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032.
Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts.
Pellowska M, Merk D, Schubert-Zsilavecz M. Advances in personalized medicine - medicinal chemistry and pharmacology of vemurafenib and ivacaftor. Pharmazie. 2013 Jul;68(7):484-91. Review. PubMed PMID: 23923627.
Banaszynski M, Kolesar JM. Vemurafenib and ipilimumab: new agents for metastatic melanoma. Am J Health Syst Pharm. 2013 Jul 15;70(14):1205-10. doi: 10.2146/ajhp120260. Review. PubMed PMID: 23820456.
Liszkay G. [Vemurafenib (Zelboraf) in the therapy of melanoma]. Magy Onkol. 2013 Jun;57(2):110-3. doi: MagyOnkol.2013.57.2.110. Epub 2013 May 14. Review. Hungarian. PubMed PMID: 23795356.
Shaw HM, Nathan PD. Vemurafenib in melanoma. Expert Rev Anticancer Ther. 2013 May;13(5):513-22. doi: 10.1586/era.13.24. Review. PubMed PMID: 23617343.
Gonzalez D, Fearfield L, Nathan P, TaniAre P, Wallace A, Brown E, Harwood C, Marsden J, Whittaker S. BRAF mutation testing algorithm for vemurafenib treatment in melanoma: recommendations from an expert panel. Br J Dermatol. 2013 Apr;168(4):700-7. doi: 10.1111/bjd.12248. Review. PubMed PMID: 23360189.
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