Dabrafenib mesylate

Biological Activity

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.

Technical Data

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.

Background References

1. A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
   Gordon et al.
   Nature, 2020;
2. Dabrafenib inhibits the growth of BRAF-WT cancers through CDK16 and NEK9 inhibition.
   Phadke et al.
   Mol.Oncol., 2018;12:74
3. 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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