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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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

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.

Takle et al (2006) Identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg.Med.Chem.Letts. 16 378.

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.

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Keywords: L-779,450, supplier, Potent, raf, kinases, inhibitors, a-raf, raf-1, L779450, Tocris Bioscience, Raf Kinase Inhibitor products

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