| Identification | Back Directory | [Name]
CEP-9722 | [CAS]
916574-83-9 | [Synonyms]
1H-Cyclopenta[a]pyrrolo[3,4-c]carbazole-1,3(2H)-dione, 4,5,6,7-tetrahydro-11-methoxy-2-[(4-methyl-1-piperazinyl)methyl]- | [Molecular Formula]
C24H26N4O3 | [MDL Number]
MFCD32641666 | [MOL File]
916574-83-9.mol | [Molecular Weight]
418.49 |
| Hazard Information | Back Directory | [Uses]
CEP-9722, the proagent of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects[1][2]. | [in vivo]
CEP-9722 (100-200 mg/kg/day; oral gavage; once daily; for 5 days a week for 4 weeks) shows dose-dependent antitumor activity in RT4 xenografts; 200 mg/kg daily is better than control and 100 mg/kg is not[1]. | Animal Model: | Nude mice bearing subcutaneous RT4 human urothelial carcinoma (UC) tumors[1] | | Dosage: | 100 or 200 mg/kg/day | | Administration: | Oral gavage; once daily; for 5 days a week for 4 weeks | | Result: | Showed dose-dependent antitumor activity in RT4 xenografts. |
| [IC 50]
PARP-1: 20 nM (IC50); PARP-2: 6 nM (IC50) | [References]
[1] Weiguo Jian, et al. Activity of CEP-9722, a poly (ADP-ribose) polymerase inhibitor, in urothelial carcinoma correlates inversely with homologous recombination repair response to DNA damage. Anticancer Drugs. 2014 Sep;25(8):878-86. DOI:10.1097/CAD.0000000000000114
[2] Ruth Plummer, et al. Phase 1 dose-escalation study of the PARP inhibitor CEP-9722 as monotherapy or in combination with temozolomide in patients with solid tumors. Cancer Chemother Pharmacol. 2014 Aug;74(2):257-65. DOI:10.1007/s00280-014-2486-9 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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