475958

c-Raf Inhibitor

The c-Raf Inhibitor controls the biological activity of c-Raf. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

• Synonym(s): c-Raf Inhibitor, 1-(3-(1,4-dihydroimidazo[4,5-c]pyrazol-5-yl)-4-methylphenyl)-3-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)urea, c-Raf Inhibitor
• Empirical Formula (Hill Notation): C₂₃H₁₉F₃N₈O
• Molecular Weight: 480.45
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: off-white
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

A cell-permeable pyrazoloimidazole phenyl urea derivative that acts as a selective type II inhibitor of c-Raf. It shows an IC₅₀ value of 50 nM in an enzymatic assay, and comparable anti-proliferative activities to sorafenib against A375P (GI ₅₀ = 2.68 µM) and WM3629 (GI₅₀ = 0.86 µM) human melanoma cell lines. When screening against a panel of 30 different kinases at a concentration of 10 µM, it exerts an inhibitory activity of 96% on c-Raf, but below 50% for most of the other kinases.

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Yu, H., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3805.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable