产品名称

西地尼布(Cediranib (AZD2171))

一般描述

Cediranib(西地尼布) is a once-daily, orally available, highly potent and selective VEGF signalling inhibitor that inhibits all three VEGF receptors.

别 称

4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline; NSC-732208

纯 度

≥98.0%(HPLC)

CAS NO.

288383-20-0

分子式

C²⁵H²⁷FN⁴O³

分子量

450.514

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Cediranib is a once-daily, orally available, highly potent and selective VEGF signalling inhibitor that inhibits all three VEGF receptors. The preclinical profile of Cediranib indicates that it has the potential to be the 'best in class' VEGF signalling inhibitor. Phase I data indicate that Cediranib is generally well tolerated, with the most common dose related adverse events being diarrhoea, hoarseness, headache and hypertension.

Cediranib (AZD2171) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFR β, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov