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Cediranib maleate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cediranib maleate图片
CAS NO:857036-77-2
包装与价格:
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

产品名称
西地尼布马来酸盐
AZD-2171 maleate
产品介绍
Cediranib maleate (AZD-2171 maleate) 是高选择性,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。
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]

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 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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7650 mL8.8249 mL17.6498 mL
5 mM0.3530 mL1.7650 mL3.5300 mL
10 mM0.1765 mL0.8825 mL1.7650 mL
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 2 mg/mL (3.53 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。