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Chemical Structure : RGB-286638
CAS No.: 784210-87-3
Catalog No.: PC-21089Not For Human Use, Lab Use Only.
RGB-286638 is a small-molecule multi-targeted cyclin-dependent kinase (CDK) inhibitor with IC50 of 1-5 nM for cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $98 | In stock | |
| 10 mg | $148 | In stock | |
| 25 mg | $258 | In stock | |
| 50 mg | $428 | In stock | |
| 100 mg | Get quote |
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RGB-286638 is a small-molecule multi-targeted cyclin-dependent kinase (CDK) inhibitor with IC50 of 1-5 nM for cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5.
RGB-286638 is less potent against cyclin H-CDK7 and cyclin D3-CDK6.
RGB-286638 also inhibits several tyrosine and serine/threonine non-CDK enzymes with IC50 of 1-50 nM, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1.
RGB-286638 potently inhibits cell growth of human p53-wt (MM.1S, MM.1R, and H929) and p53-mutant (U266, OPM1, and RPMI) MM cells with EC50 of 20-70 nM.
RGB-286638 (50nM) reduces the phosphorylation of Rb at S807/811 in MM.1S and MM.1R cells, but has no effects on p-Rb S780.
RGB-286638 induces cytotoxicity in p53 knockdown MM.1S, exhibits anti-MM activity in vivo.
| M.Wt | 618.56 | |
| Formula | C29H37Cl2N7O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N′-4-morpholinylurea hydrochloride (1:2) |
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1. Cirstea D, et al. Leukemia. 2013 Dec;27(12):2366-75.
2. van der Biessen DA, et al. Clin Cancer Res. 2014 Sep 15;20(18):4776-83.
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