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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-BS-181
BS-181

Chemical Structure : BS-181

CAS No.: 1092443-52-1

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BS-181 (BS 181, BS181)

货号: PC-43445Not 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).

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10 mg ￥980 In stock
25 mg ￥1680 In stock
50 mg ￥2680 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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).
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.

物理化学性质&存储条件

分子量 380.53
分子式 C22H32N6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Pyrazolo[1,5-a]pyrimidine-5,7-diamine, N5-(6-aminohexyl)-3-(1-methylethyl)-N7-(phenylmethyl)-

参考文献

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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