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 is an orally available PARP inhibitor. E7016 inhibits of DNA repair. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo.

E7016 (3 μM) enhances radiosensitization by 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].

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

902128-92-1

C20H19N3O3

349.38

GPI 21016

DMSO:22.5 mg/mL (64.4 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years