西地尼布马来酸盐 - CAS:857036-77-2 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	西地尼布马来酸盐
英文名称:	Cediranib maleate
别名:	西地尼布马来酸盐 AZD2171; 4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline maleate
CAS No:	857036-77-2	分子式:	C₂₅H₂₇FN₄O₃^.C₄H₄O₄	分子量:	566.59
CAS No:	857036-77-2
分子式:	C₂₅H₂₇FN₄O₃^.C₄H₄O₄
分子量:	566.59

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C10531 西地尼布马来酸盐 ≥98% (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(＞40mg/mL)

产品描述：

基本信息

产品编号：C10531
产品名称：Cediranib maleate
CAS:	857036-77-2	储存条件	粉末	-20℃	四年
分子式：	C29H31FN4O7		溶于液体	-80℃	两年
分子量	566.58			-20℃	一个月
化学名：	4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline maleate
Solubility (25°C)	体外	DMSO	100 mg/mL (176.49 mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内	现配现用
＜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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.7650mL	8.8249mL	17.6498mL
5mM	0.3530mL	1.7650mL	3.5300mL
10mM	0.1765mL	0.8825mL	1.7650mL
50mM	0.0353mL	0.1765mL	0.3530mL

生物活性

产品描述	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。
靶点/IC₅₀	VEGFR2/KDR (HUVECs)	c-Kit (HUVECs)	c-Kit (HUVECs)	VEGFR3/FLT4 (HUVECs)	VEGFR1/FLT1 (HUVECs)
靶点/IC₅₀	0.5nM	2nM	2nM	<=3nM	5nM
体外研究	In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC50 values of 0.4 and 0.5 nM, respectively. In a fibroblast/endothelial cell coculture model of vessel sprouting, Cediranib alsoreduces vessel area, length, and branching at subnanomolar concentrations.
体内研究	nce-daily oral administration of Cediranib ablates experimental (VEGF-induced) angiogenesis and inhibits endochondralossification in bone or corpora luteal development in ovary; physiologic processes that are highly dependent uponneovascularization. The growth of established human tumor xenografts (colon, lung, prostate, breast, and ovary) in athymicmice is inhibited dose-dependently by Cediranib, with chronic administration of 1.5 mg per kg per day producing statisticallysignificant inhibition in all models. A histologic analysis of Calu-6 lung tumors treated with Cediranib reveals a reduction inmicrovessel density within 52 hours that becomes progressively greater with the duration of treatment. These changes areindicative of vascular regression within tumors.
特征

推荐实验方法(仅供参考)

激酶实验：
Kinase Assay	The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit,PDGFR-α, PDGFR-β, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aur-A, and Aur-B] usingELISA methodology.

细胞实验:

Cell Assay

Proliferation of MG63 osteosarcoma cells is induced by PDGF-AA, which selectively activates PDGFR-α homodimer signaling.Cells are cultured in DMEM without phenol red containing 1% charcoal stripped FCS, 2 mM glutamine, and 1% nonessentialamino acids for 24 hours. Cediranib or vehicle is added with PDGF-AA ligand (50 ng/mL) and plates reincubated for 72 hours.Cellular proliferation is determined using a bromodeoxyuridine.

动物实验:

Animal Administration

Rats: Young female Alderley Park rats (6 weeks of age, Wistar derived, n=5) are dosed orally, once daily for 28 days withCediranib (1.25-5 mg per kg per day) or vehicle. Additional rats (five per group) are treated with Cediranib (5 mg per kg perday) or vehicle for 28 days and maintained for a further 28 days without treatment, to examine the effect of compoundwithdrawal. Histologic paraffin wax sections of the femorotibial joints and ovaries are stained with H&E. Morphometric

image analysis of femorotibial sections is done, with growth plate areas from both the femur and tibia in each joint beingcombined for an analysis of the effect of compound treatment. The area of corpora lutea in H&E-stained ovary sections issimilarly determined by morphometric analysis

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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