CDK9 PROTAC C3

Chemical Structure : CDK9 PROTAC C3

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货号: PC-24046Not For Human Use, Lab Use Only.

CDK9 PROTAC C3 is a potent and selective, oral CDK9 PROTAC degrader with DC50 of 1.09 nM in NCI-H69 cells.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

CDK9 PROTAC C3 is a potent and selective, oral CDK9 PROTAC degrader with DC50 of 1.09 nM in NCI-H69 cells.
CDK9 PROTAC C3 induces selective CRBN-mediated degradation of CDK9, decreases phosphorylation of RNA Pol II at Ser2 and Ser5, as well as reduced expression of c-Myc in NCI-H446 cells.
CDK9 PROTAC C3 exhibits excellent cytotoxicity against SCLC cell lines (NCl-H69, NCl-H146, NCl-H446, NCl-H524, and DMS114) (IC50 = 0.530 to 3.768 nM), significantly blocks the formation of malignant clone.
CDK9 PROTAC C3 strongly triggers apoptosis in NCI-H69 and NCI-H446 cells in a dose-dependent manner, attenuates the invasion of SCLCs.
CDK9 PROTAC C3 (12.5 and 25 mg/kg, QD) demonstrates significant tumor suppression (TGI = 79.2% and 84.8%, respectively) in NCI-H446 subcutaneous xenograft model.

物理化学性质&存储条件

分子量	807.78
分子式	C39H48Cl2N10O5
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	4-(2,6-Dichlorobenzamido)-N-(1-(2-(4-((4-(3-((2,6-dioxopiperidin-3-yl)amino)phenyl)piperazin-1-yl)methyl)piperidin-1-yl)acetyl)piperidin-4-yl)-1H-pyrazole-3-carboxamide

参考文献

1. Wang Y, et al. J Med Chem. 2025 Feb 2. doi: 10.1021/acs.jmedchem.4c01621.

CDK9 PROTAC C3

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CDK9 PROTAC C3

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