Chemical Structure : CDK9 PROTAC C3
CAS No.:
3039540-19-4
CDK9 PROTAC C3
Catalog No.: 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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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807.78
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Formula
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C39H48Cl2N10O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Wang Y, et al. J Med Chem. 2025 Feb 2. doi: 10.1021/acs.jmedchem.4c01621.
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