CDK inhibitor 24

Chemical Structure : CDK inhibitor 24

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货号: PC-49076Not For Human Use, Lab Use Only.

CDK inhibitor 24 is a potent inhibitor of cyclin-dependent kinases (CDKs) with IC50 of 4/20/64 nM for CDK2/9/12, respectively.

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生物&药学活性

CDK inhibitor 24 is a potent inhibitor of cyclin-dependent kinases (CDKs) with IC50 of 4/20/64 nM for CDK2/9/12, respectively.
CDK inhibitor 24 causes dephosphorylation of retinoblastoma protein and RNA polymerase II, leading to induction of apoptosis in cellular assays in lymphoma cell lines.
CDK inhibitor 24 also induces proteasome-dependent degradation of cyclin K both in vitro and in a patient-derived xenograft in vivo.
CDK inhibitor 24 has a dual mechanism of action, acting as a CDK inhibitor and as a molecular glue inducing an interaction between CDK12 and DDB1 that leads to polyubiquitination of cyclin K and its subsequent degradation.

物理化学性质&存储条件

分子量	420.539
分子式	C21H24N8S
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(4-(1H-pyrazol-1-yl)benzyl)-5-((2-aminoethyl)thio)-3-cyclobutyl-2H-pyrazolo[4,3-d]pyrimidin-7-amine

参考文献

1. Radek Jorda, et al. J. Med. Chem. 2022.

CDK inhibitor 24

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物理化学性质&存储条件

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CDK inhibitor 24

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物理化学性质&存储条件

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