CAS NO: | 857036-77-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Cediranib maleate (AZD-2171 maleate) is a highly potent, orally availableVEGFRinhibitor withIC50s of<1,<3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4,PDGFRα,PDGFRβ,c-Kit, respectively. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC50values 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[1]. | ||||||||||||||||
体内研究 (In Vivo) | 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[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 566.58 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C29H31FN4O7 | ||||||||||||||||
CAS 号 | 857036-77-2 | ||||||||||||||||
中文名称 | 西地尼布马来酸盐 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 45 mg/mL(79.42 mM) H2O : 2 mg/mL(3.53 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液
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