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857036-77-2

中文名稱 西地尼布馬來酸鹽
英文名稱 Cediranib Maleate
CAS 857036-77-2
分子式 C25H27FN4O3·C4H4O4
分子量 566.59
MOL 文件 857036-77-2.mol
更新日期 2024/12/19 15:31:43
857036-77-2 結(jié)構(gòu)式 857036-77-2 結(jié)構(gòu)式

基本信息

中文別名
西地尼布馬來酸鹽
西地尼布馬來酸鹽1
VEGFR2抑制劑(CEDIRANIB MALEATE)
英文別名
AZD 2171 Maleate
Cediranib Maleate
West to Ni BuMa Maleate
Cediranib Maleate(AZD-2171)
AZD-2171 MALEATE
AZD 2171 MALEATE
Cediranib maleate (AZD-2171 maleate
4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline maleate
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)198.3-200.08 °C (polymorph)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO:72.5(Max Conc. mg/mL);127.96(Max Conc. mM)
Water:2.0(Max Conc. mg/mL);3.53(Max Conc. mM)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
西地尼布馬來酸鹽價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-13049西地尼布馬來酸鹽
Cediranib maleate
857036-77-25mg500元
2024/11/08HY-13049西地尼布馬來酸鹽
Cediranib maleate
857036-77-210mM * 1mLin DMSO623元
2024/11/08HY-13049西地尼布馬來酸鹽
Cediranib maleate
857036-77-210mg750元

常見問題列表

生物活性
Cediranib maleate (AZD-2171 maleate) 是高選擇性,有口服活性的 VEGFR2 抑制劑,對(duì)Flt1,KDR,F(xiàn)lt4,PDGFRα,PDGFRβ,c-Kit的 IC50 值分別為小于1, 小于3,5,5,36,2nM。
靶點(diǎn)
TargetValue
VEGFR2/KDR
(HUVECs)
0.5 nM
c-Kit
(HUVECs)
2 nM
c-Kit
(HUVECs)
2 nM
VEGFR3/FLT4
(HUVECs)
<=3 nM
VEGFR1/FLT1
(HUVECs)
5 nM
體外研究

In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC 50 values 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.

體內(nèi)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.

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