| 产品描述: | Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively. |
| 靶点: |
Flt-1:5 nM (IC50);KDR:1 nM (IC50);Flt-4:3 nM (IC50);PDGFRα:36 nM (IC50);PDGFRβ:5 nM (IC50);c-Kit:2 nM (IC50) |
| 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 |
| 参考文献: |
1. Wedge SR, et al. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res, 2005, 65(10), 4389-4400. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
-20℃;充氩 |
| 配置溶液浓度参考: |
|
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 |
| 50 mM |
0.035 ml |
0.176 ml |
0.353 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |