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.
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- CAS No.: 2248068-54-2
- Formule: C28H25ClF3N3O
- Masse moléculaire:511.97
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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 |
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| 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 (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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Masse moléculaire 511.97
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Poloppin II Related Classifications
HY-125220 Related Classifications
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