857036-77-2
857036-77-2 结构式
基本信息
西地尼布马来酸盐1
VEGFR2抑制剂(CEDIRANIB MALEATE)
Cediranib Maleate
West to Ni BuMa Maleate
Cediranib Maleate(AZD-2171)
AZD-2171 MALEATE
AZD 2171 MALEATE
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
物理化学性质
Water:2.0(Max Conc. mg/mL);3.53(Max Conc. mM)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-13049 | 西地尼布马来酸盐 Cediranib maleate | 857036-77-2 | 5mg | 500元 |
| 2024/04/30 | HY-13049 | 西地尼布马来酸盐 Cediranib maleate | 857036-77-2 | 10mM * 1mLin DMSO | 623元 |
| 2024/04/30 | HY-13049 | 西地尼布马来酸盐 Cediranib maleate | 857036-77-2 | 10mg | 750元 |
常见问题列表
| 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.