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• 产品描述： 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 IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity

• 靶点： Molecular Glues;Integrin;Integrin

• 体外研究：
  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

• 体内研究：
  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. Animal Model: Six-week-old female nude mice (KSN mice, WiDr-induced angiogenesis model) Dosage: 50, 100, 200 mg/kg Administration: p.o. ; twice daily for 14 days from 2 days after inoculation of the tumor cells Result: The antitumor effect was dose-dependent at 50, 100, and 200 mg/kg, and the tumor growth rates were 52%, 46%, and 27%, respectively.

• 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.973 ml	14.865 ml	29.729 ml
  5 mM	0.595 ml	2.973 ml	5.946 ml
  10 mM	0.297 ml	1.486 ml	2.973 ml
  50 mM	0.059 ml	0.297 ml	0.595 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *