CDK2 degrader 8
CDK2 degrader 8 is a selective cyclin-dependent kinase 2 (CDK2) degrader. CDK2 degrader 8 can be used in studies related to CDK2 degradation and HR+ HER2- breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3099145-52-2
- Formula: C25H19ClF3N5O5
- Molecular Weight:561.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
CDK2 |
In Vitro
CDK2 degrader 8 (compound 1) induces CDK2 degradation in CDK2-HiBiT HEK293 cells after 24 h of treatment, with a Dmax of 64.8%. In the corresponding GSPT1 Live-cell HiBiT assay, the Dmax of GSPT1 is only 3.3%, demonstrating selectivity for CDK2 degradation[1].
CDK2 degrader 8 (1 μM; 60 min) exhibits a CLint of 46.6 μL/min/mg in the human liver microsome stability assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice, 6-8 weeks old, approximately 18-22 g[1]
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Dosage:100 mg/kg
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Administration:i.p.; once daily for 21 days
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Result:Inhibited tumor growth compared with the vehicle group.
Achieved 50% TGI at Day 21.
Chemical Information
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CAS No. 3099145-52-2
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Molecular Weight 561.90
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Formula C25H19ClF3N5O5
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SMILES
FC(F)(OC1=CC=C(C2=NN=C(O2)NC3(CC3)C4=CC(Cl)=C5CN(C(C5=C4)=O)C6CCC(NC6=O)=O)C=C1)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)