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S80060

E-3810

源叶(MedMol) 95%
  • 英文名:
  • E-3810
  • 别名:
  • CS-0782; Lucitanib; QC-4603; UNII-PP449XA4BH; E-3810 amine; 6-[[7-[(1-aminocyclopropyl)methoxy]-6-methoxy-4-quinolyl]oxy]-N-methyl-naphthalene-1-carboxamide; 6-(7-((1-Aminocyclopropyl)methoxy)-6-metho
  • CAS号:
  • 1058137-23-7
  • 分子式:
  • C26H25N3O4
  • 分子量:
  • 443.49
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80060-5mg 95% ¥860.00元 10 - - - EA 加入购物车
源叶(MedMol) S80060-10mg 95% ¥1420.00元 9 - - - EA 加入购物车
源叶(MedMol) S80060-50mg 95% ¥3800.00元 2 - - - EA 加入购物车
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参考文献

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  • 提示:详情请下载说明书。
  • 产品描述: Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
  • 靶点: VEGFR1:7 nM (IC50);VEGFR2:25 nM (IC50);VEGFR3:10 nM (IC50);FGFR1:17.5 nM (IC50);FGFR2:82.5 nM (IC50);VEGFR;FGFR
  • 体内研究:
    Lucitanib (E-3810), at oral dosing of 20 mg/kg for 7 consecutive days, completely inhibits (P<0.01) the bFGF induced angiogenic response compare with the response in vehicle-treated mice. Lucitanib (E-3810) shows a broad spectrum of activity, being active in all the xenografts tested (HT29 colon carcinoma, A2780 ovarian carcinoma, A498, SN12K1, and RXF393 renal carcinomas) with dose-dependent inhibition of tumor growth. E-3810 significantly delays growth during treatment, but tumors resume their growth when treatment is suspended; in a few cases, tumor regression is observed. The activity of Lucitanib (E-3810) given at the doses of 15 mg/kg is tested on MDA-MB-231 breast cancer transplanted subcutaneously, at a late stage, when tumor masses reach 350 to 400 mg. This tumor xenograft is very sensitive to Lucitanib (E-3810), with complete tumor stabilization lasting throughout the 30-day treatment. As in other tumor models, tumors re-grow after withdrawal of Lucitanib (E-3810) at a rate similar to control tumors
  • 参考文献:
    1. Bello E, et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. 2. Colzani M, et al. Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509. 3. Bello E, et al. The tyrosine kinase inhibitor E-3810 combined with NSC 125973 inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131-40
  • 溶解性: DMSO  :  ≥  20.83  mg/mL  (46.97  mM)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.255 ml 11.274 ml 22.548 ml
    5 mM 0.451 ml 2.255 ml 4.51 ml
    10 mM 0.225 ml 1.127 ml 2.255 ml
    50 mM 0.045 ml 0.225 ml 0.451 ml
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