E7016 GPI 21016|cas:902128-92-1|西域试剂

E7016 GPI 21016,98.46%

产品编号：Bellancom-13540| CAS NO：902128-92-1| 分子式：C₂₀H₁₉N₃O₃| 分子量：349.38

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-13540		￥5000.00	杭州北京（现货）
Bellancom-13540		￥8500.00	杭州北京（现货）

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E7016 GPI 21016

产品介绍

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 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.

体外研究

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⁺.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (71.56 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。