AG-024104
AG-024104 is a CDK inhibitor with Ki values of 2.3 nM (CDK1/cyclinB), 1.8 nM (CDK2/cyclinA), and 0.67 nM (CDK4/cyclinD). AG-024104 functionally inhibits kinase activity of CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD. AG-024104 serves as a negative control for peripheral leukocyte toxicity studies in preclinical development.
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- No. CAS: 750575-23-6
- Fòrmula: C24H28F2N6O4S2
- Peso molecular:566.64
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Almacenamiento:
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Actividad biológica
Descripciòn
In Vitro
AG-024104 potently inhibits purified CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD enzymes with Ki values of 2.3 nM, 1.8 nM, and 0.67 nM, respectively[1].
AG-024104 (4 days) inhibits HCT-116 colorectal carcinoma cell growth with an IC50 of 51 nM[1].
AG-024104 (24 h) induces cytotoxicity in human PBMCs and monkey PBLs with TC50 values of 7.2 μM and 4.0 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 colorectal carcinoma cells
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Concentration:concentrations to achieve 50% growth inhibition (IC50 determination)
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Incubation Time:4 days
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Result:Inhibited HCT-116 cell growth with an IC50 of 51 nM.
Parmacokinetics
| Species | Dose | Route | AUC0-24 | T1/2 |
|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.v. | 2.7 μg·h/mL | 1.4 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (male, ~10 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.v.; single bolus injection over 2-3 min
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Result:Remained at ~93% of pre-treatment levels 24 hours post-dose.
Chemical Information
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No. CAS 750575-23-6
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Peso molecular 566.64
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Fòrmula C24H28F2N6O4S2
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SMILES
O=C(C=1SC(=NC1N)NC2CCN(CC2)S(=O)(=O)C3=CN=C(OCCN(C)C)C=C3)C=4C(F)=CC=CC4F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AG-024104 Related Classifications
HY-123238 Related Classifications
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