CDK2-IN-60
CDK2-IN-60 is an orally active, ATP-competitive selective CDK2 inhibitor with a Ki of 77 pM. CDK2-IN-60 has high selectivity for both CDK4 and CDK1. CDK2-IN-60 blocks G1/S cell cycle progression to suppress proliferation of CCNE1-amplified tumor cells. CDK2-IN-60 serves as a lead chemical probe for investigating CCNE1-amplified cancers and CDK4/6 inhibitor-resistant HR-positive breast cancer.
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- CAS No.: 2922859-30-9
- Formule: C18H26N6O3
- Masse moléculaire:374.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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CDK2 77 pM (Ki) |
CDK2-IN-60 (Compound19) (30 min) potently inhibits CDK2 kinase with a Ki value of 77 pM and exhibits 584-fold and 47-fold selectivity over CDK4 and CDK1 respectively[1].
CDK2-IN-60 (16 h) displays robust antiproliferative activity against CCNE1-amplified OVISE ovarian cancer cells with an EdU IC50 of 0.03 μM and 50-fold cellular selectivity over CCNE1-low SKOV3 cells[1].
CDK2-IN-60 (1 μM; 0-3 h) possesses excellent metabolic stability in human primary hepatocytes with undetectable hepatic clearance in vitro[1].
CDK2-IN-60 (5 μM; 60-80 min) shows moderate membrane permeability in MDCK cells and is identified as a substrate of human P-gp and BCRP efflux transporters via bidirectional permeability tests[1].
CDK2-IN-60 (5 μM; 6 h) presents moderate plasma protein binding measured by in vitro equilibrium dialysis assay[1].
CDK2-IN-60 selectively binds CDK2 Lys89, confirmed by molecular dynamics and kinase co-crystal structures[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | Vss | T1/2 | AUC0-∞ | F | CLplasma | CLrenal | Bioavailability | Tmax |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 47 mL/min/kg | 1.1 L/kg | 0.3 h | / | / | / | / | / | / |
| Mice[1] | 5 mg/kg | p.o. | / | / | / | 2.9 μM·h | 61 % | / | / | / | / |
| Mice[1] | 50 mg/kg | p.o. | / | / | / | 28.7 μM·h | / | / | / | / | / |
| Rat[1] | 3 mg/kg | i.v. | / | / | / | / | / | 56 mL/min/kg | 9.7 mL/min/kg | / | / |
| Rat[1] | 5 mg/kg | p.o. | / | / | / | / | / | / | / | 67 % | 1.4 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female SCID.bg (C.B-17 SCID.bg) mice aged (6-8 weeks with an average weight of 24-26 g) were inoculated with OVCAR-3 X2.1 ovarian adenocarcinoma cells[1]
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Dosage:10 mg/kg, 30 mg/kg, 60 mg/kg
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Administration:p.o., once daily, for 21 days
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Result:Exhibited dose-dependent tumor growth inhibition, with a maximum TGI of 79% at the highest tested dose.
Did not significantly affect mouse body weight.
Chemical Information
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CAS No. 2922859-30-9
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Masse moléculaire 374.44
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Formule C18H26N6O3
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SMILES
O=C(NC(C)(C)C)O[C@H](CC1)C[C@H]1C2=CC(NC(C=C3)=NN(C)C3=O)=NN2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK2-IN-60 Related Classifications
HY-184649 Related Classifications
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