Dabrafenib mesylate New
Chemical Name: N-[3-[5-(2-Aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide methanesulfonate
Biological ActivityPotent 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.
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.
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Gordon et al.
Dabrafenib inhibits the growth of BRAF-WT cancers through CDK16 and NEK9 inhibition.
Phadke et al.
Discovery of Dabrafenib: a selective inhibitor of Raf kinases with antitumor activity against B.Raf-driven tumors.
Rheault et al.
ACS Med Chem Lett, 2013;4:358
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