Vemurafenib
Vemurafenib is a first generation selective B-Raf inhibitor that has been approved for clinical use in treating unresectable or metastatic melanoma; it exhibits anticancer chemotherapeutic activity. Vemurafenib binds the ATP-binding domain of mutant (V600E) B-Raf, present in many cancer subtypes, to inhibit downstream MEK and ERK signaling. This compound inhibits MAPK signaling and cell cycle progression in cells expressing mutant (V600E) B-Raf, but may increase MAPK signaling in cells expressing WT B-Raf. Subjects undergoing treatment with Vemurafenib have potential to develop verrucal keratosis and cutaneous squamous cell carcinoma as side effects. Vemurafenib is currently under examination as a potential treatment against tumors expressing H-Ras mutations as well.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18978783
| Cas No. |
1029872-54-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C23H18ClF2N3O3S |
| Formula Wt. |
489.92 |
| Chemical Name |
N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide |
| IUPAC Name |
N-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide |
| Synonym |
PLX-4032; RG7204; RO5185426 |
| Appearance |
White to off white powder |
Anforth R, Blumetti TC, Clements A, et al. Systemic Retinoids for the Chemoprevention of Cutaneous Squamous Cell Carcinoma and Verrucal Keratosis in a Cohort of Patients on BRAF inhibitors. Br J Dermatol. 2013 Jul 20. PMID: 23870055.
Beck D, Niessner H, Smalley KS, et al. Vemurafenib potently induces endoplasmic reticulum stress-mediated apoptosis in BRAFV600E melanoma cells. Sci Signal. 2013 Jan 29;6(260):ra7. PMID: 23362240.
Huang T, Karsy M, Zhuge J, et al. B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 25;6:30. PMID: 23617957.
