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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CDK inhibitor E9
CDK inhibitor E9

Chemical Structure : CDK inhibitor E9

CAS No.: 2020052-55-3

CDK inhibitor E9 (E9)

货号: PC-63235Not For Human Use, Lab Use Only.

CDK inhibitor E9 is a novel CDK inhibitor that can overcomes ABC-mediated resistance of THZ1, functions as a potent, non-covalent inhibitor of CDK9 and a covalent inhibitor of CDK12.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CDK inhibitor E9 is a novel CDK inhibitor that can overcomes ABC-mediated resistance of THZ1, functions as a potent, non-covalent inhibitor of CDK9 and a covalent inhibitor of CDK12.
CDK inhibitor E9 does not serve as a substrate for either ABCB1 or ABCG2, while avoiding ABC transporter-mediated efflux.
CDK inhibitor E9 decreases the phosphorylated and total RNAPII in THZ1R NB and lung cancer cells (IC50=8-40 nM), accompanied by decreased MYC and MCL1 expression, exerts its cytotoxic effects through covalent modification of cysteine 1039 of CDK12.

物理化学性质&存储条件

分子量 434.544
分子式 C24H30N6O2
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

(S)-N-(3-((3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)phenyl)acrylamide

参考文献

1. Gao Y, et al. Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5.

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