Dabrafenib mesylate

Name: Dabrafenib mesylate
Brand: Tocris Bioscience
SKU: 7223

Tocris Bioscience, part of Bio-Techne | Catalog # 7223

COA / SDS

Potent and selective B-Raf, CDK16 and NEK9 inhibitor; anticancer; also targets human proteins in the SARS-CoV-2 interactome

Key Product Details

Description:	Potent and selective B-Raf, CDK16 and NEK9 inhibitor; anticancer; also targets human proteins in the SARS-CoV-2 interactome
Chemical Name:	N-[3-[5-(2-Aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide methanesulfonate
Purity:	≥98% (HPLC)
Molecular Weight:	615.66

View Full Technical Details for Dabrafenib mesylate

Technical Data
Citations

Biological Activity for Dabrafenib mesylate

Dabrafenib mesylate is a potent and selective Raf kinase inhibitor (IC₅₀ values are 0.8, 3.2 and 5.0 nM for B-Raf^V600E, wild-type B-Raf and c-Raf, respectively). Exhibits selectivity for B-Raf over a panel of 270 other kinases. Arrests cell cycle in the G₁ phase and inhibits growth of B-Raf^V600E mutant melanoma and colon cancer cells in vitro and in vivo. Orally bioavailable. Also inhibits NEK9 (IC₅₀ <10 nM) and CDK16. Identified as targeting human host proteins that interact with SARS-CoV-2.

Compound Libraries for Dabrafenib mesylate

Dabrafenib mesylate is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for Dabrafenib mesylate

M. Wt	615.66
Formula	C₂₃H₂₀F₃N₅O₂S₂.CH₃SO₃H
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1195768-06-9
PubChem ID	44516822
InChi Key	YKGMKSIHIVVYKY-UHFFFAOYSA-N
Smiles	CS(O)(=O)=O.CC(C)(C1=NC(C2=C(C(NS(=O)(C3=C(C=CC=C3F)F)=O)=CC=C2)F)=C(C4=NC(N)=NC=C4)S1)C

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 Dabrafenib mesylate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	30.78	50

Preparing Stock Solutions for Dabrafenib mesylate

The following data is based on the product molecular weight 615.66.

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
0.5 mM	3.25 mL	16.24 mL	32.49 mL
2.5 mM	0.65 mL	3.25 mL	6.50 mL
5 mM	0.32 mL	1.62 mL	3.25 mL
25 mM	0.06 mL	0.32 mL	0.65 mL

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References for Dabrafenib mesylate

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

Gordon A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. Nature 2020 PMID: 32353859
Rheault Discovery of Dabrafenib: a selective inhibitor of Raf kinases with antitumor activity against B.Raf-driven tumors. ACS Med Chem Lett 2013 PMID: 24900673
Phadke Dabrafenib inhibits the growth of BRAF-WT cancers through CDK16 and NEK9 inhibition. Mol.Oncol. 2018 PMID: 29112787