Poloppin II
Poloppin II is an orally active PBD inhibitor that blocks the binding of phosphopeptide substrates to PLK1/PLK2 PBD, with IC50 values of 41 µM and 105 µM for human PLK1/PLK2 PBD, respectively. Poloppin II binds to PLK4 PBD to inhibit PLK4-dependent mitotic functions. Poloppin II can be used in research on kras-mutant colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 2248068-54-2
- Formula: C28H25ClF3N3O
- Molecular Weight:511.97
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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
Biological Activity
Description
IC50 & Target
[1]|
PLK1 PBD 41 μM (IC50) |
PLK2 PBD 105 μM (IC50) |
PLK4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
61 nM
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Induction of mitotic arrest in human HeLa cells assessed by anti-phospho-histone H3 (Ser10) intensity after 16 hrs incubation.
Induction of mitotic arrest in human HeLa cells assessed by anti-phospho-histone H3 (Ser10) intensity after 16 hrs incubation.
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28807782 |
In Vitro
Poloppin II (16 h) induces mitotic arrest in HeLa cells with EC50 61 nM (MI EC50 0.069 μM; 81% max)[1].
Poloppin II (1 h at 22°C) inhibits phosphopeptide binding to PLK1 PBD with IC50 41 μM and to PLK2 PBD with IC50 105 μM in FP assays[1].
Poloppin II (100 μM; 1 h at 37°C; 3 min over 42-66°C gradient) engages PLK1 and PLK4 in NanoLuc thermal shift assays in HeLa cells[1].
Poloppin II is inactive against hERG and stable in human and mouse hepatocytes[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:athymic nude (male)[1]
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Dosage:50 mg/kg; 200 mg/kg
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Administration:p.o. once every three days; p.o. single dose (PD-sampling cohort)
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Result:Was well tolerated at 50 mg/kg with no adverse health observations or recorded weight loss.
Reduced the growth of xenografted HCT116 tumours at 50 mg/kg.
Increased phospho-Ser10 histone H3 levels within 24 hours compared with vehicle controls.
Chemical Information
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CAS No. 2248068-54-2
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Molecular Weight 511.97
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Formula C28H25ClF3N3O
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SMILES
O=C(NCCN(C)C)C1=CC=C(C=C1)C2=CC=C(C=3C=CC(Cl)=CC3)N2C=4C=CC=CC4C(F)(F)F
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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)
Poloppin II Related Classifications
HY-125220 Related Classifications
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