西地尼布马来酸盐  ≥98%

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包装规格:5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介:一种高选择性,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。
溶解性:溶于DMSO(>40mg/mL)
储备液保存:-80°C, 6 months -20°C, 1 month (sealed storage, away from moisture)
体内实验:1、请依序添加每种溶剂: PBS Solubility: 2 mg/mL (3.53 mM); 澄清溶液; 超声助溶 (<60°C) <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
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)
体外研究:In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC50 values of 0.4and 0.5nM, 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.
保存条件:-20℃
注意事项:1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。