PLK2-IN-1
PLK2-IN-1 is a selective PLK2 inhibitor (IC50 0.78 μM). PLK2-IN-1 induces Apoptosis and cell cycle arrest, reduces AKT and mTOR phosphorylation, and decreases Cyclin E expression as well as downregulates the CDK2/Rb/E2F1 axis. PLK2-IN-1 inhibits tumor growth in colorectal cancer xenograft models. PLK2-IN-1 can be used for research on colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C28H36N6O
- Molecular Weight:472.63
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PLK2 0.78 μM (IC50) |
PLK1 >10 μM (IC50) |
PLK3 >10 μM (IC50) |
PLK4 >10 μM (IC50) |
CDK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| SW480 | GI50 |
1.67 μM
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Antiproliferative activity against human SW480 colorectal cancer cells assessed as GI50 for viability reduction incubated 72 hrs by CellTiter-Glo assay.
Antiproliferative activity against human SW480 colorectal cancer cells assessed as GI50 for viability reduction incubated 72 hrs by CellTiter-Glo assay.
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42700477 |
| HT-29 | GI50 |
3.72 μM
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Antiproliferative activity against human HT29 colorectal cancer cells assessed as GI50 for viability reduction incubated 72 hrs by CellTiter-Glo assay.
Antiproliferative activity against human HT29 colorectal cancer cells assessed as GI50 for viability reduction incubated 72 hrs by CellTiter-Glo assay.
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42700477 |
In Vitro
PLK2-IN-1 (2-3 weeks) inhibits anchorage-independent colony formation of SW480 and HT29 colorectal cancer cells[1].
PLK2-IN-1 (10 μM) reduces phosphorylation of AKT and mTOR in SW480 cells[1].
PLK2-IN-1 (1 μM; 30 min) showed good microsomal stability in mouse and rat liver microsomes[1].
PLK2-IN-1 does not significantly inhibit CYP enzymes, with IC50 values >10 μM for CYP2C9, CYP2C19, CYP2D6, and CYP3A4, and 7.95 μM for CYP1A2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW480 and HT29
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Concentration:10 μM (% inhibition); varying concentrations (GI50)
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Incubation Time:72 h
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Result:SW480 cells showed 106.00% inhibition at 10 μM; GI50 was 1.67 μM.
HT29 cells showed 97.33% inhibition at 10 μM; GI50 was 3.72 μM.
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Cell Line:SW480 and HT29
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced apoptosis in 39.17% of SW480 cells and 26.97% of HT29 cells at 10 μM.
Increased cleaved caspase-3 and cleaved PARP protein levels compared with control in both cell lines.
Parmacokinetics
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 nu/nu (male, 6 weeks at purchase, acclimated for one week)[1]
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Dosage:7.5 mg/kg; 15 mg/kg
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Administration:i.p.; once daily; 21 days
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Result:Produced tumor growth inhibition (TGI) rates of 39.33% at 7.5 mg/kg and 69.37% at 15 mg/kg in the SW480 xenograft model.
At 15 mg/kg, two mice exhibited tumor regression, with tumor sizes decreasing below their initial measurements.
Immunohistochemical analysis showed that compound 11 decreased Ki-67 expression by 42.07% relative to the vehicle group and downregulated cyclin E expression by 34.97% compared with the vehicle group.
- Western Blot
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Molecular Weight 472.63
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Formula C28H36N6O
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SMILES
CCN(N=C1C2=CC(C=CC=C3)=C3C=C2)C4=C1C=NC(NCCOCCN5C(CC)CCCC5)=N4
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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)
PLK2-IN-1 Related Classifications
HY-189637 Related Classifications
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