| Description | E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 inhibits of DNA repair. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo. |
| In vitro | E7016（3 μM）通过增加进入有丝分裂灾难的细胞数量而非增加进入细胞凋亡的细胞数量，提高了放射增敏效应[1]。E7016通过模拟NAD+[2]，抑制PARP。 |
| In vivo | 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]. |
| Synonyms | GPI 21016 |
| molecular weight | 349.38 |
| Molecular formula | C20H19N3O3 |
| CAS | 902128-92-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 22.5 mg/mL (64.4 mM), Sonication and heating to 60℃ are recommended. |
| References | 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. |