E7016

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

E7016 can enhance tumor cell radiosensitivity through the inhibition of DNA repair.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.E7016 inhibits PARP by mimicking NAD+.Apoptosis Analysis Cell Line:The U251 human glioblastoma cell line Concentration:3 μM Incubation Time:6 hours prior to irradiation and were stained at 24 and 72 h postirradiation Result:The number of cells in mitotic catastrophe was significantly greater in the E7016-treated irradiated cells than in cells that received radiation only at 24 hours postirradiation.

E7016 has antitumor efficacy in murine xenograft studies.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 Temozolomide and irradiation in vivo.Animal Model:Four- to six-week-old female nude mice Dosage:40 mg/kg Administration:Oral gavage Result:E7016 enhanced the radiation/Temozolomide (3 mg/kg orally)-induced tumor growth delay of U251 xenografts.

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Cell Cycle/DNA Damage

PARP

PARP

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902128-92-1

349.38

C20H19N3O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 25 mg/mL (71.56 mM; 超声助溶 (<60°C)

OC1CCN(Cc2ccc3oc4cccc5c4c(n[nH]c5=O)c3c2)CC1

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(-20℃)

With Ice Pack

≥ 2 years