Dabrafenib mesylate

Pricing Availability   Qty
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)

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-RafV600E, 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-RafV600E 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
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 Data for Dabrafenib mesylate

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 6.5 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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Product Datasheets for Dabrafenib mesylate

References for Dabrafenib mesylate

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

Phadke et al (2018) Dabrafenib inhibits the growth of BRAF-WT cancers through CDK16 and NEK9 inhibition. Mol.Oncol. 12 74 PMID: 29112787

Gordon et al (2020) A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. Nature 583 PMID: 32353859

Rheault et al (2013) Discovery of Dabrafenib: a selective inhibitor of Raf kinases with antitumor activity against B.Raf-driven tumors. ACS Med Chem Lett 4 358 PMID: 24900673

If you know of a relevant reference for Dabrafenib mesylate, please let us know.

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Citations for Dabrafenib mesylate

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