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Submit ReviewDabrafenib mesylate
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 |
| 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 Data for Dabrafenib mesylate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 | 6.5 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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