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E7016
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
E7016图片
CAS NO:902128-92-1
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
E7016 (GPI 21016) 是一种口服有效的 PARP 抑制剂。E7016 可以通过抑制 DNA 修复来增强肿瘤细胞在体内外的放射敏感性。E7016 用作一种潜在的抗肿瘤剂。
Cas No.902128-92-1
别名GPI 21016
分子式C20H19N3O3
分子量349.38
溶解度DMSO : 25 mg/mL (71.56 mM; ultrasonic and warming and heat to 60℃)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent[1][2].

E7016 can enhance tumor cell radiosensitivity through the inhibition of DNA repair[1].E7016 (3 μM)-mediated radiosensitization occurs through an increase in the number of cells undergoing mitotic catastrophe and not an increase in the number of cells undergoing apoptosis[1].E7016 inhibits PARP by mimicking NAD+[2].

E7016 has antitumor efficacy in murine xenograft studies[1].Administration of E7016 (40 mg/kg; oral gavage) to mice bearing U251 xenografts enhances the effectiveness of the Temozolomide/radiation combination[1]. Mice treated with E7016/irradiation/Temozolomide have an additional growth delay of six days compared with the combination of Temozolomide and irradiation in vivo[1].

[1]. Andrea L Russo, et al. In vitro and in vivo radiosensitization of glioblastoma cells by the poly (ADP-ribose) polymerase inhibitor E7016. Clin Cancer Res. 2009 Jan 15;15(2):607-12.
[2]. W George Lai, et al. A Baeyer-Villiger oxidation specifically catalyzed by human flavin-containing monooxygenase 5. Drug Metab Dispos. 2011 Jan;39(1):61-70.