CDK12-IN-E9 | CDK12 inhibitor | Probechem Biochemicals

Chemical Structure : CDK12-IN-E9

CAS No.: 2020052-55-3

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CDK12-IN-E9 (E9, CDK12 inhibitor E9 S-isomer)

货号: PC-60490Not For Human Use, Lab Use Only.

CDK12 inhibitor E9 S-isomer (E9, CDK12-IN-E9) is a clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux.

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10 mg	￥5280	In stock
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生物&药学活性

CDK12 inhibitor E9 S-isomer (E9, CDK12-IN-E9) is a clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux.
CDK12-IN-E9 dose-dependently decreases phosphorylated and total RNAPII in THZ1R NB and lung cancer models, competed strongly with bio-THZ1 for binding to CDK12 at low nanomolar ranges, but not CDK7 (>1 uM).
CDK12-IN-E9 exerts its cytotoxic effects through covalent modification of cysteine 1039 of CDK12.
CDK12-IN-E9 shows more potent antiproliferative activity in THZ1R NB and lung cancer cells with IC50 ranging from 8 to 40 nM than ribociclib, palbociclib, and AZD5438.

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. 2017 Dec 15. pii: S2451-9456(17)30424-5.

CDK12-IN-E9 (E9, CDK12 inhibitor E9 S-isomer)

生物&药学活性

物理化学性质&存储条件

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CDK12-IN-E9 (E9, CDK12 inhibitor E9 S-isomer)

生物&药学活性

物理化学性质&存储条件

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