CAIX/CDK-2-IN-1
CAIX/CDK-2-IN-1 is a dual-acting inhibitor of carbonic anhydrase IX (CA IX) and cyclin-dependent kinase-2 (CDK-2) with IC50 values of 0.29 μM and 0.32 μM. The zein nanoparticls of CAIX/CDK-2-IN-1 can induce cancer cells apoptosis. CAIX/CDK-2-IN-1 can be used for the research of cancer, such as lung cancer.
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- Fòrmula: C25H18ClN5O4S3
- Peso molecular:584.09
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
CA IX 0.29 μM (IC50) |
CDK2 0.32 μM (IC50) |
Caspase-8 |
Caspase-9 |
Caspase 3 |
Bax |
Bcl-2 |
In Vitro
CAIX/CDK-2-IN-1 (Compound 5c) (Zein NPs) (10 μM) shows cell growth inhibition rate (GI%) of 94.8% in A549 cells, while its free base only has GI% of 3%[1].
CAIX/CDK-2-IN-1 (Zein NPs) (48 h) induce apoptosis, upregulates the expression of P53, Bax, PUMA and Caspase-3/8/9 genes and downregulates Bcl-2 in A549 cells[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:BALB/c mice with Urethane (HY-B1207)-induced lung cancer[1]
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Dosage:6 mg/kg (Zein NPs)
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Administration:Intranasally administration, daily from week 17 to 20
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Result:Reduced the lung index (relative lung weight from 2.91 to 1.35) .
Decreased lung weight (from 567.4±26.7 mg to 298.6±16.4 mg).
Inhibited the protein expression of hCA IX, hCA XII and CDK-2 by 45%, 58% and 46% respectively.
Improved the 20-week survival rate of mice to 40%.
Chemical Information
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Peso molecular 584.09
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Fòrmula C25H18ClN5O4S3
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SMILES
ClC1=CC=C(C2=NC(N=C(SCC(NC3=CC=C(S(=O)(N)=O)C=C3)=O)NC4=O)=C4C(C5=CC=CS5)=C2)C=C1
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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)
CAIX/CDK-2-IN-1 Related Classifications
HY-179022 Related Classifications
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