PARP-2-IN-3
PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability.
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- CAS. Nr.: 2915650-86-9
- Formel: C20H20ClN3O3
- Molecular Weight:385.84
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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PARP-2 0.07 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MCF7 | IC50 |
6.05 μM
Compound: 175a
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
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[PMID: 38838546] |
| MDA-MB-231 | IC50 |
6.14 μM
Compound: 175a
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Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
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[PMID: 38838546] |
PARP-2-IN-3 (Compound 12) (24 h) shows cytotoxic activities with IC50s of 6.14±0.5 μM and 6.05±0.4 μM against MDA-MB-231 and MCF-7, respectively[1].
PARP-2-IN-3 (6.05 μM; 24 h) arrests cell cycle at G2/M phase, and induces apoptosis and necrosis in MCF-7 cells[1].
PARP-2-IN-3 fills the space inside the PARP-2 pocket in a manner similar to Olaparib (HY-10162)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 and MCF-7
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Concentration:
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Incubation Time:24 h
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Result:Displayed remarkable cytotoxic activities with IC50s of 6.14±0.5 μM and 6.05±0.4 μM against MDA-MB-231 and MCF-7, respectively.
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Cell Line:MCF-7
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Concentration:6.05 μM
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Incubation Time:24 h
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Result:The percentage of cells in pre-G1 phase increased from 1.85% to 33.47%, while in G2/M phase increased from 11.84% to 32.04%. The percentage of cells in S phase slightly decreased from 29.95% to 26.18% and in G0/G1 phase decreased from 58.21% to 41.78%.
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Cell Line:MCF-7
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Concentration:6.05 μM
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Incubation Time:24 h
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Result:Induced an early apoptotic effect 22.52% and late apoptotic effect 3.72% in comparison to the untreated negative control MCF-7 cells which induced an early and late apoptotic effect 0.37% and 0.33%, respectively.
Chemical Information
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CAS. Nr. 2915650-86-9
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Molecular Weight 385.84
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Formel C20H20ClN3O3
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SMILES
O=C(NC1=CC=C(C2=NC3=CC(Cl)=CC=C3O2)C=C1)CCN4CCOCC4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PARP-2-IN-3 Related Classifications
HY-151625 Related Classifications
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