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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- 화학식: C25H18ClN5O4S3
- 분자량:584.09
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
More
Biological Activity
제품 설명
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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분자량 584.09
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)