CDK4/6-IN-28
CDK4/6-IN-28 is a potent, orally active, and selective CDK4/6 inhibitor IC50 values of 14.02 and 10.03 nM, respectively. CDK4/6-IN-28 inhibits breast cancer cell colony formation, migration, and proliferation. CDK4/6-IN-28 induces G1-phase cell cycle arrest and apoptosis in breast cancer cells. CDK4/6-IN-28 exhibits tumor inhibitory activity in breast cancer xenograft mouse models. CDK4/6-IN-28 can be used for the research of breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3110098-09-1
- Formula: C25H29N7
- Molecular Weight:427.54
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
All Caspase Isoforms
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Biological Activity
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CDK6 10.03 nM (IC50) |
CDK4 14.02 nM (IC50) |
BCL2 |
Caspase 3 |
CDK4/6-IN-28 (compound 3c) (72 h) potently inhibits the proliferation of MCF-7, 4T1, and MDA-MB-231 cells with IC50 values of 0.11, 0.21, and 0.12 μM, respectively, with favorable selectivity over non-cancerous 3T3 cells (IC50 = 4.64 μM)[1].
CDK4/6-IN-28 (1-2 μM; 7 days) suppresses colony information of MCF-7 breast cancer cells in a concentration-dependent manner[1].
CDK4/6-IN-28 (1-2 μM; 24 h) inhibits the migratory capacity of MCF-7 breast cancer cells in a concentration-dependent manner[1].
CDK4/6-IN-28 (1-2 μM; 12-24 h) induces apoptosis, reduces mitochondrial membrane potential, and increases ROS production in MCF-7 breast cancer cells in a concentration-dependent manner[1].
CDK4/6-IN-28 (1-2 μM; 24 h) induces concentration-dependent G1 phase cell cycle arrest in MCF-7 breast cancer cells[1].
CDK4/6-IN-28 (1-4 μM; 24 h) blocks the CDK4/6-Rb-E2F signaling pathway in MCF-7 breast cancer cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 breast cancer cells
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Concentration:1, 2 μM
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Incubation Time:7 days
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Result:Reduced both colony number and size in a concentration-dependent manner compared to control.
Showed inhibitory efficacy comparable to positive control Abemaciclib (HY-16297) at 2 μM.
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Cell Line:MCF-7 breast cancer cells
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Concentration:1, 2 μM
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Incubation Time:24 h
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Result:Suppressed MCF-7 cell migration in a concentration-dependent manner, as shown by impaired wound closure compared to control.
Showed anti-migratory efficacy comparable to positive control Abemaciclib at 2 μM.
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Cell Line:MCF-7 breast cancer cells
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Concentration:1, 2 μM
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Incubation Time:12 h
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Result:Induced concentration-dependent apoptotic features including nuclear condensation, chromatin condensation, and apoptotic body formation.
Caused a concentration-dependent decrease in red JC-1 fluorescence and increase in green fluorescence, with effect comparable to Abemaciclib at 2 μM.
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Cell Line:MCF-7 breast cancer cells
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Concentration:1, 2 μM
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Incubation Time:24 h
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Result:Caused a concentration-dependent increase in the proportion of MCF-7 cells in the G1 phase, with 2 μM resulting in 65.13% of cells in G1.
Induced concentration-dependent apoptosis, with 1 μM causing a total apoptosis rate of 13.36% and 2 μM causing a total apoptosis rate of 19.14%.
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Cell Line:MCF-7 breast cancer cells
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Caused a concentration-dependent decrease in phosphorylated Rb (p-Rb) levels.
Downregulated total Rb, E2F1, and Cyclin-D1 expression in a concentration-dependent manner.
Showed inhibitory effects on p-Rb and E2F1 expression comparable to 4 μM Abemaciclib at 4 μM.
CDK4/6-IN-28 (60-120 mg/kg; p.o.; daily; 7 days) exhibits favorable biosafety in healthy KM mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu nude mice (female, 4-6 weeks old, 18-20 g) injected with MCF-7 cells[1]
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Dosage:25; 50 mg/kg
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Administration:p.o.; every other day; 14 days
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Result:Achieved a tumor inhibition rate of 30.41% at 25 mg/kg.
Achieved a tumor inhibition rate of 45.20% at 50 mg/kg.
Maintained stable body weight throughout treatment.
Showed no significant differences in total protein, ALT, lactate dehydrogenase, or urea levels compared to control; AST and creatinine levels were slightly lower than control, while alkaline phosphatase levels were slightly higher.
Showed no significant tissue damage to heart, liver, spleen, lung, or kidney via HE staining.
Induced dose-dependent decreases in Bcl2, Ki67, and PCNA expression, and increases in Caspase3 expression.
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Animal Model:KM mice (female, 4-5 weeks old, 18-22 g)[1]
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Dosage:60 ; 120 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Increased alanine aminotransferase (ALT) levels from 100 U/L to 111.67 U/L, and aspartate aminotransferase (AST) levels from 40.67 U/L to 46 U/L at 120 mg/kg, with both values remaining within physiological reference ranges and ALT/AST ratios below 2.6.
Showed extremely mild cellular degeneration and edema in liver and kidney at 120 mg/kg, with no severe damage to heart, lung, or spleen.
Chemical Information
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CAS No. 3110098-09-1
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Molecular Weight 427.54
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Formula C25H29N7
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SMILES
CC(C=C1)=CC=C1C2=NC3=CC=NN3C(NC4=CC=C(CN5CCN(CC)CC5)C=N4)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK4/6-IN-28 Related Classifications
HY-183771 Related Classifications
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