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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-ZLC853
ZLC853

Chemical Structure : ZLC853

CAS No.: 3097996-25-0

ZLC853 (ZLC-853)

货号: PC-28745Not For Human Use, Lab Use Only.

ZLC853 is a potent, selective, and orally bioavailable covalent inhibitor of CDK12/13 with IC50 of 40.0 nM and 18.2 nM respectively, inhibits VCaP cell proliferation with IC50 of 13.7 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ZLC853 is a potent, selective, and orally bioavailable covalent inhibitor of CDK12/13 with IC50 of 40.0 nM and 18.2 nM respectively, inhibits VCaP cell proliferation with IC50 of 13.7 nM.
ZLC853 covalently binds and modifies Cys 1039 in CDK12 and Cys 1017 in CDK13.
ZLC853 exhibits high kinase selectivity for CDK12 and CDK13, shows 16- and 36-fold selectivity over other CDKs with exception of CDK7 (IC50=81.75 nM).
ZLC853 does not engage CDK7 covalently in cells.
ZLC853 (100 nM) inhibits Ser 2 phosphorylation of RNA polymerase II, suppresses transcription of DDR genes, and induces apoptosis in VCaP cells.
ZLC853 (5 and 10 mg/kg, p.o., q.d.) inhibits prostate cancer growth in VCaP CRPC mouse model.

物理化学性质&存储条件

分子量 697.84
分子式 C38H45F2N9O2
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

N-(2-(4-(dimethylamino)piperidin-1-yl)-5-(3-((S)-1-(4-fluorophenyl)ethyl)-1-((1r,4S)-4-(quinazolin-2-ylamino)cyclohexyl)ureido)pyridin-3-yl)-2-fluoroacrylamide

参考文献

1. Zhou K, et al. Acta Pharm Sin B. 2026 Nov;16(11):7554-7572.

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