西地尼布马来酸盐
西地尼布马来酸盐 性质
| 熔点 | 198.3-200.08 °C (polymorph) |
|---|---|
| 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) |
西地尼布马来酸盐 用途与合成方法
| 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.
西地尼布马来酸盐 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-01-25 | HY-13049 | 西地尼布马来酸盐 | 857036-77-2 | 5mg | 500 |
| 2024-01-25 | HY-13049 | 西地尼布马来酸盐 | 857036-77-2 | 10mM * 1mLin DMSO | 623 |
