CEP-9722

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CEP-9722 

CEP-9722 是 CEP-8983 的前药,是一种选择性且具有口服活性的PARP-1PARP-2 抑制剂,IC50 分别为 20 nM 和 6 nM。CEP-9722 具有抗癌作用。

CEP-9722

CEP-9722 Chemical Structure

CAS No. : 916574-83-9

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生物活性

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].

IC50 & Target[2]

PARP-1

20 nM (IC50)

PARP-2

6 nM (IC50)

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

418.49

Formula

C24H26N4O3

CAS 号

916574-83-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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