CDK4-IN-5
CDK4-IN-5 is a potent, orally active and selective CDK4 inhibitor. CDK4-IN-5 suppresses CDK4 expression and downregulates the CDK4/CyclinD1 complex. CDK4-IN-5 induces G0/G1 phase cell cycle arrest in bladder cancer cells via CyclinD1 expression suppression. CDK4-IN-5 selectively exerts activity against bladder cancer cells. CDK4-IN-5 can be used for the research of bladder cancer.
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- 화학식: C28H40O6
- 분자량:472.61
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보관:
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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
Cdk4/cyclin D1 |
In Vitro
CDK4-IN-5 (compound 2a) (0.016-50 μM; 72 h) potently inhibits the viability of T24 and 5637 bladder cancer cells with IC50 values of 0.44 μM and 0.49 μM, respectively, while demonstrating favorable selectivity over normal SV-HUC-1 cells (IC50 = 4.51 μM)[1].
CDK4-IN-5 (0.1 μM; 24-72 h) exerts a time-dependent inhibitory effect on the proliferation of T24 and 5637 bladder cancer cells[1].
CDK4-IN-5 (150-300 nM; 10-14 days) potently and durably suppresses colony formation of T24 and 5637 bladder cancer cells in a dose-dependent manner[1].
CDK4-IN-5 (600-1200 nM; 24 h) induces dose-dependent G0/G1 phase cell cycle arrest in T24 and 5637 bladder cancer cells[1].
CDK4-IN-5 (120-3000 nM; 48 h) dose-dependently downregulates CDK4 and CyclinD1 protein expression in T24 bladder cancer cells[1].
CDK4-IN-5 stably binds to the ATP-binding pocket of CDK4, with a most favorable binding energy of -10.1 kcal/mol at the CDK4 site[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T24, 5637 cells
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Concentration:150; 300 nM
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Incubation Time:10-14 days
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Result:Inhibited colony formation of T24 and 5637 cells in a dose-dependent manner.
Showed a marked inhibitory effect in both T24 and 5637 cells.
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Cell Line:T24, 5637 cells
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Concentration:0.1 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Showed no significant inhibition at 24 h.
Decreased OD values by 37.41% in T24 cells and 50.90% in 5637 cells by 48 h.
Reduced OD values further to 45.47% in T24 cells and 51.89% in 5637 cells by 72 h.
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Cell Line:T24, 5637 cells
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Concentration:600; 1200 nM
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Incubation Time:24 h
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Result:Induced accumulation of cells in the G0/G1 phase with concurrent reduction in S phase population.
Increased G0/G1 phase percentage from 57.16% to 81.22% in T24 cells and from 44.10% to 63.55% in 5637 cells at 600 nM.
Further increased G0/G1 phase percentage to 83.12% in T24 cells and 66.74% in 5637 cells at 1200 nM, with S phase fractions decreasing to 9.17% in T24 cells and 26.99% in 5637 cells.
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Cell Line:human bladder cancer T24 cells
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Concentration:120; 600; 3000 nM
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Incubation Time:48 h
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Result:Significantly reduced CDK4 expression in a dose-dependent manner.
Decreased CyclinD1 levels in a dose-dependent manner.
Parmacokinetics
Chemical Information
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분자량 472.61
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화학식 C28H40O6
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SMILES
C[C@@]1(CCC([C@@H](CCC2[C@H]3C)C)[C@]42OO1)O[C@H]4O[C@H]3OC(C(C)C5=CC=C(C=C5)CC(C)C)=O
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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)
CDK4-IN-5 Related Classifications
HY-183297 Related Classifications
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