E7820|289483-69-8|(ER68203-00)-陌孚医药/Medlife

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E7820 (Synonyms: ER68203-00)

目录号: PL07446 纯度: ≥99%

CAS No. :289483-69-8

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中文名称	E7820
中文别名	3-氰基-N-(3-氰基-4-甲基-1H-吲哚-7-基)苯磺酰胺
英文名称	E7820
英文别名	Benzenesulfonamide,3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)-;E 7820;E-7820;AC1L52N5;ER68203-00;KB-76741;NSC719239;NSC-719239;SureCN1581157;E7820;3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)benzenesulfonamide;TVH5K7949N;N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzene-sulfonamide;N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzenesulfonamide;Benzenesulfonamide, 3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)-;3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)benzene-1-sulfonamide;O6M;3-Cyano-N-(3-cyano-4-methyl-1H-indole-7-yl)benzensulfonamide;3-Cyan-N-(3-cyan-4-methyl-1H-indol-7-yl)benzolsulfonamid;3-Cyano-N-(3-cyano-4-méthyl-1H-indol-7-yl)benzènesulfonamide;3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)-benzenesulfonamide;Boc-Met-OSu;BS-16799;http:////www.amadischem.com/proen/581203/
Cas No.	289483-69-8
分子式	C₁₇H₁₂N₄O₂S
分子量	336.37
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

E7820 (ER68203-00) 是一种具有口服活性芳香族磺酰胺衍生物，是一种独特的血管生成 (angiogenesis) 抑制剂，可抑制内皮上整合素 α2 (integrin alpha2) 亚基的表达。E7820 抑制大鼠主动脉血管生成，IC₅₀ 为 0.11 μg/ml。E7820 调节 α-1，α-2，α-3 和 α-5 整联素 mRNA 表达。具有抗血管生成和抗肿瘤活性。

生物活性

E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC 50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.

性状

Solid

体外研究(In Vitro)

E7820 (ER68203-00) inhibits both bFGF- and VEGF-driven ube formation of human umbilical vascular endothelial cell (HUVEC) in a dose-dependent manner with IC50 of 0.20 and 0.24 μg/ml, respectively.
E7820 inhibits proliferation of HUVEC induced by either bFGF or VEGF in serum-free medium (SFM). The IC50 values are 0.10 and 0.081 μg/ml, respectively. Antiproliferative activity of E7820 against both WiDr and LoVo cells is very weak compared with that against HUVEC. The values of IC50 were 29 and 15 μg/ml, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

E7820 (ER68203-00) (50-200 mg/kg; p.o. ; twice daily for 14 days) delays the growth of WiDr cells inoculated s.c..
E7820 (200-400 mg/kg; p.o.;once daily for 4 days) potently inhibits WiDr-induced angiogenesis. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Funahashi Y, et al. Sulfonamide derivative, E7820, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. Cancer Res. 2002;62(21):6116-6123.
[2]. Ito K, et al. Enhanced anti-angiogenic effect of E7820 in combination with erlotinib in epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer xenograft models. Cancer Sci. 2014;105(8):1023-1031.

溶解度数据	In Vitro: DMSO : 100 mg/mL (297.29 mM; Need ultrasonic)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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