中文名 | 西地尼布马来酸盐 |
英文名 | Cediranib Maleate |
别名 | 马来酸盐西地尼布 西地尼布马来酸盐 西地尼布马来酸盐1 化合物EHT 1864 VEGFR2抑制剂(CEDIRANIB MALEATE) |
英文别名 | AZD-2171 MALEATE AZD 2171 MALEATE AZD 2171 Maleate Cediranib Maleate West to Ni BuMa Maleate Cediranib Maleate(AZD-2171) Cediranib maleate (AZD-2171 maleate 4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline maleate (Z)-but-2-enedioic acid,4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline |
CAS | 857036-77-2 |
化学式 | C25H27FN4O3·C4H4O4 |
分子量 | 566.59 |
熔点 | 198.3-200.08 °C (polymorph) |
存储条件 | Room Temprature |
物化性质 | 生物活性 Cediranib maleate (AZD-2171 maleate) 是高选择性,有口服活性的 VEGFR2 抑制剂,对Flt1,KDR,Flt4,PDGFRα,PDGFRβ,c-Kit的 IC50 值分别为小于1, 小于3,5,5,36,2nM。 |
体外研究 | In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC 50 values of 0.4 and 0.5 nM, respectively. In a fibroblast/endothelial cell coculture model of vessel sprouting, Cediranib also reduces vessel area, length, and branching at subnanomolar concentrations. |
体内研究 | Once-daily oral administration of Cediranib ablates experimental (VEGF-induced) angiogenesis and inhibits endochondral ossification in bone or corpora luteal development in ovary; physiologic processes that are highly dependent upon neovascularization. The growth of established human tumor xenografts (colon, lung, prostate, breast, and ovary) in athymic mice is inhibited dose-dependently by Cediranib, with chronic administration of 1.5 mg per kg per day producing statistically significant inhibition in all models. A histologic analysis of Calu-6 lung tumors treated with Cediranib reveals a reduction in microvessel density within 52 hours that becomes progressively greater with the duration of treatment. These changes are indicative of vascular regression within tumors. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.765 ml | 8.825 ml | 17.65 ml |
5 mM | 0.353 ml | 1.765 ml | 3.53 ml |
10 mM | 0.176 ml | 0.882 ml | 1.765 ml |
5 mM | 0.035 ml | 0.176 ml | 0.353 ml |
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