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Submit ReviewVemurafenib
Description: Potent BRAF and CRAF inhibitor
Chemical Name: N-[3-[[5-(4-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide
Purity: ≥98% (HPLC)
Biological Activity for Vemurafenib
Vemurafenib is a potent inhibitor of BRAFV600E, C-Raf and wild type B-Raf (IC50 values are 13-31 nM, 6.7-48 nM and 100-160 nM, respectively. Vemurafenib also inhibits SRMS, ACK1 KHS1, FGR (IC50 values are 18 nM, 19 nM, 51 nM and 63 nM, respectively). Vemurafenib shows antitumor activity and induces autophagy in BRAF-mutant thyroid cancer cells.
Compound Libraries for Vemurafenib
Vemurafenib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for Vemurafenib
| M. Wt | 489.92 |
| Formula | C23H18ClF2N3O3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 918504-65-1 |
| PubChem ID | 42611257 |
| InChI Key | GPXBXXGIAQBQNI-UHFFFAOYSA-N |
| Smiles | O=C(C1=CNC2=NC=C(C=C21)C=3C=CC(Cl)=CC3)C=4C(F)=CC=C(NS(=O)(=O)CCC)C4F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Vemurafenib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.99 | 100 |
Preparing Stock Solutions for Vemurafenib
The following data is based on the product molecular weight 489.92. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.04 mL | 10.21 mL | 20.41 mL |
| 5 mM | 0.41 mL | 2.04 mL | 4.08 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.04 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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Product Datasheets for Vemurafenib
References for Vemurafenib
References are publications that support the biological activity of the product.
Wang et al (2017) Targeting autophagy sensitizes BRAF-mutant thyroid cancer to vemurafenib. J.Clin.Endocrinol.Metab. 102 634 PMID: 27754804
Ibrahim et al (2013) Chapter twenty-six - case history: vemurafenib, a potent, selective, and first-in-class inhibitor of mutant BRAF for the treatment of metastatic melanoma. Annu.Rep.Med.Chem. 48 435
Davis and Schlessinger (2012) The genesis of zelboraf: targeting mutant B-Raf in melanoma. J.Cell.Biol. 199 15 PMID: 23027900
If you know of a relevant reference for Vemurafenib, please let us know.
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Keywords: Vemurafenib, Vemurafenib supplier, BRAF, kinases, inhibitors, inhibits, potent, BRAFV600E, CRAF, B-raf, c-raf, autophagy, antitumor, Raf, Kinase, 7309, Tocris Bioscience
Citations for Vemurafenib
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