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Chemical Structure : PF-00477736
CAS No.: 952021-60-2
Catalog No.: PC-35602Not For Human Use, Lab Use Only.
PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $198 | In stock | |
| 10 mg | $328 | In stock | |
| 25 mg | $528 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM).
PF-00477736 displays <100-fold selectivity over VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret, and Yes in a panel of >100 protein kinases.
PF-00477736 abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin; enhances the antitumor activity of gemcitabine in a dose-dependent manner in xenografts.
| M.Wt | 419.489 | |
| Formula | C22H25N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-2-amino-2-cyclohexyl-N-(5-(1-methyl-1H-pyrazol-4-yl)-1-oxo-2,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide |
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1. Blasina A, et al. Mol Cancer Ther. 2008 Aug;7(8):2394-404.
2. Zhang C, et al. Clin Cancer Res. 2009 Jul 15;15(14):4630-40.
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