Vemurafenib

Name: Vemurafenib
Brand: Tocris Bioscience
SKU: 7309

Tocris Bioscience, part of Bio-Techne | Catalog # 7309

Citations (2)

COA / SDS

Potent BRAF and CRAF inhibitor

Key Product Details

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)
Molecular Weight:	489.92

View Full Technical Details for Vemurafenib

Technical Data
Citations

Biological Activity for Vemurafenib

Vemurafenib is a potent inhibitor of BRAF^V600E, 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 for Vemurafenib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	0.20 mL	1.02 mL	2.04 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

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References for Vemurafenib

References are publications that support the biological activity of the product.

Ibrahim 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.
Davis and Schlessinger The genesis of zelboraf: targeting mutant B-Raf in melanoma. J.Cell.Biol. 2012 PMID: 23027900
Wang Targeting autophagy sensitizes BRAF-mutant thyroid cancer to vemurafenib. J.Clin.Endocrinol.Metab. 2017 PMID: 27754804