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。
| 生物活性 | E7016 (GPI 21016) is an orally availablePARPinhibitor. 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]. |
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体外研究
(In Vitro) | 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].
Apoptosis Analysis[1] | 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. |
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体内研究
(In Vivo) | 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].
| Animal Model: | Four- to six-week-old female nude mice[3] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(71.56 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.8622 mL | 14.3111 mL | 28.6221 mL | | 5 mM | 0.5724 mL | 2.8622 mL | 5.7244 mL | | 10 mM | 0.2862 mL | 1.4311 mL | 2.8622 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.25 mg/mL (3.58 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (3.58 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.25 mg/mL (3.58 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (3.58 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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