2. Cell Cycle/DNA Damage Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. CDK Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism Bcl-2 Family Caspase
  4. 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.

CDK4/6-IN-28

CDK4/6-IN-28 Chemical Structure

CAS No. : 3110098-09-1

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CDK4/6-IN-28 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

IC50 & Target[1]

CDK6

10.03 nM (IC50)

CDK4

14.02 nM (IC50)

BCL2

 

Caspase 3

 

In Vitro

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.

CDK4/6-IN-28 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MCF-7 breast cancer cells
Concentration: 1, 2 μM
Incubation Time: 7 days
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.

Cell Migration Assay [1]

Cell Line: MCF-7 breast cancer cells
Concentration: 1, 2 μM
Incubation Time: 24 h
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.

Apoptosis Analysis[1]

Cell Line: MCF-7 breast cancer cells
Concentration: 1, 2 μM
Incubation Time: 12 h
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.

Cell Cycle Analysis[1]

Cell Line: MCF-7 breast cancer cells
Concentration: 1, 2 μM
Incubation Time: 24 h
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%.

Western Blot Analysis[1]

Cell Line: MCF-7 breast cancer cells
Concentration: 1, 2, 4 μM
Incubation Time: 24 h
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.
In Vivo

CDK4/6-IN-28 (compound 3c) (25-50 mg/kg; p.o.; every other day; 14 days) inhibits tumor growth in MCF-7 xenograft mice[1].
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.

Animal Model: BALB/c-nu nude mice (female, 4-6 weeks old, 18-20 g) injected with MCF-7 cells[1]
Dosage: 25; 50 mg/kg
Administration: p.o.; every other day; 14 days
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.
Animal Model: KM mice (female, 4-5 weeks old, 18-22 g)[1]
Dosage: 60 ; 120 mg/kg
Administration: p.o.; daily; 7 days
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.
Molecular Weight

427.54

Formula

C25H29N7
CAS No.
SMILES

CC(C=C1)=CC=C1C2=NC3=CC=NN3C(NC4=CC=C(CN5CCN(CC)CC5)C=N4)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CDK4/6-IN-28 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK4/6-IN-283110098-09-1CDKApoptosisReactive Oxygen Species (ROS)Mitochondrial MetabolismBcl-2 FamilyCaspaseCyclin dependent kinasebreast cancer cellsG1-phase cell cycle arrestCDK4CDK6MDA-MB-231MCF-7apoptosis4T1breast cancer xenograft mouse models3T3 cellsInhibitorinhibitorinhibit

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