CDK2 degrader 10
CDK2 degrader 10 is an orally active, cereblon-based molecular glue degrader targeting CDK2, with a DC50 of 120 nM. CDK2 degrader 10 forms a ternary complex with cereblon and CDK2 via a non-canonical recruitment mode, thereby driving CDK2 degradation through the ubiquitin-proteasome system. CDK2 degrader 10 inhibits retinoblastoma protein phosphorylation, induces G1/S cell cycle arrest, and suppresses CDK2-dependent cell proliferation. CDK2 degrader 10 can be used in studies related to CDK2-dependent cancers.
For research use only. We do not sell to patients.
- Formula: C22H24FN5O5
- Molecular Weight:457.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CDK2 120 nM (DC50) |
CDK2 degrader 10 (Compound B12) (16 nM-10 μM; 2-24 h) induces dose- and time-dependent degradation of CDK2, but does not induce GSPT1 degradation, in MCF7 cells[1].
CDK2 degrader 10 (16 h) mediates the formation of the CRBN-CDK2 ternary complex in HEK293T cells, with an EC50 of 226 nM[1].
CDK2 degrader 10 (1-10 μM; 24 h) induces mild G0/G1 cell cycle arrest in MDA-MB-157 cells[1].
CDK2 degrader 10 (1-10 μM; 24 h) inhibits CDK2-mediated Rb phosphorylation in MDA-MB-157 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 cells
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Concentration:16, 80, 400 nM, 2, 10 μM (dose-response); 10 μM (time-course)
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Incubation Time:24 h (dose-response); 2, 4, 6, 16, 24 h (time-course)
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Result:Induced dose-dependent degradation of CDK2 in MCF7 cells, with noticeable reduction at concentrations as low as 80 nM after 24 h.
Showed no measurable degradation of GSPT1 across all tested concentrations.
Revealed progressive CDK2 degradation over 24 h of treatment with 10 μM CDK2 degrader 10 (Compound B12).
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Cell Line:MDA-MB-157 cells
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Concentration:1 and 10 μM
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Incubation Time:24 h
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Result:Associated with a modest increase in the G0/G1 cell population and a reduction in the S-phase population relative to untreated control cells.
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Cell Line:MDA-MB-157 cells
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Concentration:1 and 10 μM
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Incubation Time:24 h
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Result:Reduced CDK2 protein levels and modestly suppressed pRb-S807/811 and pRb-S780 levels relative to untreated control cells at 10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOG mice (female, MCF7 breast cancer xenograft, preimplanted with 17 β-estradiol pellets 1 day prior to cell inoculation)[1]
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Dosage:100 mg/kg (i.p. administration); 100 mg/kg (p.o. administration)
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Administration:i.p.; BID; 3 days; p.o.; BID; 3 days
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Result:Reduced intratumoral CDK2 protein levels to approximately 40% of vehicle-treated control levels.
Reduced intratumoral CDK2 protein levels to approximately 60% of vehicle-treated control levels.
Chemical Information
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Molecular Weight 457.45
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Formula C22H24FN5O5
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SMILES
FC1=C(N=CN(C2=O)C3CCC(NC3=O)=O)C2=CN=C1CNC(OCC4CC5(C4)CCC5)=O
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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)
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