916574-83-9

Name	CEP-9722
CAS	916574-83-9
Molecular Formula	C24H26N4O3
MDL Number	MFCD32641666
Molecular Weight	418.49
MOL File	916574-83-9.mol

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]-

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Chemical Properties

Boiling point	664.1±55.0 °C(Predicted)
density	1.374±0.06 g/cm3(Predicted)
pka	15.72±0.20(Predicted)

Hazard Information

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

Spectrum Detail

CEP-9722(916574-83-9)¹HNMR

Supplier

Shanghai Biopharmaleader Co., Ltd.

Telephone+86 18721201413

Websitehttp://www.biopharmaleader.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Shanghai Amole Biotechnology Co., Ltd.

Telephone13370042665 18916960931

Websitehttps://www.amole.com.cn/

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