Potent, ATP-competitive Raf kinase inhibitor (IC50 = 10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively. Suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
References are publications that support the biological activity of the product.
White (2003) Small-molecule inhibitors of signal transduction pathways in leukemia therapeutics: how to assess selectivity for malignant signals. Leukemia 17 1759 PMID: 12970775
Shelton et al (2003) Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation. Leukemia 17 1765 PMID: 12970777
Takle et al (2006) Identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg.Med.Chem.Letts. 16 378
Röring et al (2012) Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling. EMBO J. 31 2629 PMID: 22510884
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Keywords: L-779,450, L-779,450 supplier, Potent, raf, kinases, inhibitors, inhibits, a-raf, raf-1, L779450, Raf, Kinase, 3185, Tocris Bioscience
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