Vemurafenib

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Cat.No. 7309 - Vemurafenib | C23H18ClF2N3O3S | CAS No. 918504-65-1
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)
Datasheet
Citations
Reviews
Literature (3)

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.

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.

Select a batch to recalculate based on the batch molecular weight:
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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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


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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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Currently there are no citations for Vemurafenib. Do you know of a great paper that uses Vemurafenib from Tocris? Please let us know.

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Literature in this Area

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