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Chemical Structure : BS-181 hydrochloride
CAS No.: 1397219-81-6
Catalog No.: PC-43446Not For Human Use, Lab Use Only.
BS-181 is a potent, selective CDK7 inhibitor with IC50 of 21 nM, 40-fold selectivity over CDK2/cycE and no significant activity against CDK1/cycB, CDK4/cycD1, CDK5/p35NCK, CDK6/cycD1, and CDK9/cycT (IC50>1 uM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $118 | In stock | |
| 25 mg | $188 | In stock | |
| 50 mg | $298 | In stock | |
| 100 mg | $488 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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BS-181 hydrochloride is a potent, selective CDK7 inhibitor with IC50 of 21 nM, 40-fold selectivity over CDK2/cycE and no significant activity against CDK1/cycB, CDK4/cycD1, CDK5/p35NCK, CDK6/cycD1, and CDK9/cycT (IC50>1 uM).
BS-181 promotes cell cycle arrest and inhibits cancer cell growth in a panel of cell lines representing a range of tumor types (IC50=1.5 to 37 uM).
BS-181 inhibits the phosphorylation of CDK7 substrates, inhibits phosphorylation of the RNA polymerase II COOH-terminal domain (CTD) at P-Ser5 (IC50=9 uM), inhibits RB phosphorylation at Ser795 and Ser821 (IC50=15 uM).
BS-181 induces apoptosis in vitro, and shows antitumor effects in vivo.
| M.Wt | 416.99 | |
| Formula | C22H33ClN6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Pyrazolo[1,5-a]pyrimidine-5,7-diamine, N5-(6-aminohexyl)-3-(1-methylethyl)-N7-(phenylmethyl)-, hydrochloride (1:1) |
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1. Ali S, et al. Cancer Res. 2009 Aug 1;69(15):6208-15.
2. Kelso TW, et al. Mol Cell Biol. 2014 Oct 1;34(19):3675-88.
3. Wang BY, et al. Drug Des Devel Ther. 2016 Mar 16;10:1181-9.
4. Li B, et al. Cancer Res. 2017 Jul 15;77(14):3834-3845.
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