西地尼布马来酸盐
中文名称 | 西地尼布马来酸盐 |
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中文同义词 | 西地尼布马来酸盐;西地尼布马来酸盐1;VEGFR2抑制剂(CEDIRANIB MALEATE);马来酸盐西地尼布;化合物EHT 1864 |
英文名称 | Cediranib Maleate |
英文同义词 | Cediranib Maleate;AZD 2171 Maleate;West to Ni BuMa Maleate;Cediranib Maleate(AZD-2171);4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline maleate;Cediranib maleate (AZD-2171 maleate;AZD-2171 MALEATE;AZD 2171 MALEATE |
CAS号 | 857036-77-2 |
分子式 | C25H27FN4O3·C4H4O4 |
分子量 | 566.59 |
EINECS号 | |
相关类别 | 抗肿瘤类药物及免疫抑制剂;医药类;细胞生物学试剂;原料药及中间体类;科研出口类;API;API |
Mol文件 | 857036-77-2.mol |
结构式 |
西地尼布马来酸盐 性质
熔点 | 198.3-200.08 °C (polymorph) |
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储存条件 | Store at -20°C |
溶解度 | DMSO:72.5(最大浓度 mg/mL);127.96(最大浓度 mM) 水:2.0(最大浓度 mg/mL);3.53(最大浓度 mM) |
形态 | 固体 |
颜色 | 白色至米白色 |
Target | Value |
VEGFR2/KDR
(HUVECs) | 0.5 nM |
c-Kit
(HUVECs) | 2 nM |
c-Kit
(HUVECs) | 2 nM |
VEGFR3/FLT4
(HUVECs) | <=3 nM |
VEGFR1/FLT1
(HUVECs) | 5 nM |
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-13049 | 西地尼布马来酸盐 Cediranib maleate | 857036-77-2 | 5mg | 500元 |
2024/08/19 | HY-13049 | 西地尼布马来酸盐 Cediranib maleate | 857036-77-2 | 10mM * 1mLin DMSO | 623元 |