R&D Systems Inc. Tocris Bioscience Boston Biochem

L-779,450

Cat. No. 3185

L-779,450 C20H14ClN3O [303727-31-3]

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Chemical Name: 2-Chloro-5-[2-Phenyl-5-(4-pyridinyl)-1H-imidazol-4-yl]phenol

Biological Activity

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.

Technical Data

M.Wt:
347.8
Formula:
C20H14ClN3O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
303727-31-3

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

Shelton et al (2003) Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation. Leukemia 17 1765. PMID: 12970777.

White (2003) Small-molecule inhibitors of signal transduction pathways in leukemia therapeutics: how to assess selectivity for malignant signals. Leukemia 17 1759. PMID: 12970775.

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.

If you know of a relevant citation for this product please let us know.

View Related Products by Target

Keywords: L-779,450, supplier, Potent, raf, kinases, inhibitors, a-raf, raf-1, L779450

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