E7016(Synonyms: GPI 21016)

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E7016 (Synonyms: GPI 21016) 纯度: 98.46%

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(Synonyms: GPI 21016)

E7016 Chemical Structure

CAS No. : 902128-92-1

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E7016 相关产品

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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[1][2].

IC50 & Target[1]

PARP

 

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

349.38

Formula

C20H19N3O3
CAS 号

902128-92-1
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°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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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.

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