E7016|902128-92-1|(GPI 21016)-陌孚医药/Medlife

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E7016 (Synonyms: GPI 21016)

目录号: PL08896 纯度: ≥98%

CAS No. :902128-92-1

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中文名称	E7016
中文别名	10-((4-hydroxypiperidin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one
英文名称	E7016
英文别名	E7016
Cas No.	902128-92-1
分子式	C₂₀H₁₉N₃O₃
分子量	349.38
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情

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.

性状

Solid

IC50 & Target[1][2]

PARP

体外研究(In Vitro)

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

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

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)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 25 mg/mL (71.56 mM; ultrasonic and warming and heat to 60°C)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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