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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.
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 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 |
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