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CEP-9722

Names

[ CAS No. ]:
916574-83-9

[ Name ]:
CEP-9722

Biological Activity

[Description]:

CEP-9722, the prodrug 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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> PARP
Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

PARP-1:20 nM (IC50)

PARP-2:6 nM (IC50)


[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.

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H26N4O3

[ Molecular Weight ]:
418.49

Related Compounds