PARP-2/1-IN-2
PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with Kis of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC50 of 3 nM in a cell based assay of PARP activity.
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- CAS. Nr.: 912444-01-0
- Formel: C13H16N4O
- Molecular Weight:244.29
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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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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PARP2 2 nM (Ki) |
PARP1 5 nM (Ki) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL6J mice, Cisplatin (HY-17394) and Oxaliplatin (HY-17371)-induced painful neuropathy models[1]
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Dosage:25 mg/kg or 50 mg/kg
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Administration:Intraperitoneal injection, two days prior to treatment with Cisplatin or oxaliplatin, with administration continuing by i.p. injection along with the Cisplatin or oxaliplatin regimen (5 days, followed by 5 days of rest, for two weekly cycles)
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Result:Does not attenuate Cisplatin and Oxaliplatin-induced body weight loss. Does not Affect the decline in exploratory behavior associated with Cisplatin and Oxaliplatin Treatment. Attenuates mechanical allodynia in Cisplatin and Oxaliplatin-induced neuropathy. Attenuates thermal hyperalgesia in Cisplatin-induced neuropathy. Attenuates cold hyperalgesia associated with Oxaliplatin-induced neuropathy.
Chemical Information
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CAS. Nr. 912444-01-0
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Molecular Weight 244.29
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Formel C13H16N4O
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SMILES
NC(C1=C2C(N=C([C@]3(C)CCCN3)N2)=CC=C1)=O
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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-2/1-IN-2 Related Classifications
HY-105253 Related Classifications
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