Dabrafenib mesylate

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Cat.No. 7223 - Dabrafenib mesylate | C23H20F3N5O2S2.CH3SO3H | CAS No. 1195768-06-9
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)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

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.

Technical Data

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

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

Preparing Stock Solutions

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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References

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 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


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Keywords: Dabrafenib mesylate, Dabrafenib mesylate supplier, potent, selective, B-Raf, kinase, inhibitors, CDK16, NEK9, inhibits, chemotherapeutic, anticancer, SARS-CoV-2, COVID-19, severe, acute, respiratory, syndrome, Raf, Kinase, Cyclin-dependent, 7223, Tocris Bioscience

Citations for Dabrafenib mesylate

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