E7016 (Synonyms: GPI 21016) |
| Catalog No.GC64209 |
E7016(GPI 21016)은 경구로 사용 가능한 PARP 억제제입니다. E7016은 DNA 복구 억제를 통해 시험관 내 및 생체 내에서 종양 세포 방사선 감수성을 향상시킬 수 있습니다. E7016은 잠재적인 항암제로 작용합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 902128-92-1
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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