产品名称

Tivozanib (AV-951)

一般描述

Tivozanib is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.

别 称

1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea; KRN-951

纯 度

≥98.0%(HPLC)

CAS NO.

475108-18-0

分子式

C²²H¹⁹ClN⁴O⁵

分子量

454.86

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

≥15mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Tivozanib is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities. Tivozanib binds to and inhibits VEGFRs 1, 2 and 3, which may result in the inhibition of endothelial cell migration and proliferation, inhibition of tumor angiogenesis and tumor cell death. VEGFR tyrosine kinases, frequently overexpressed by a variety of tumor cell types, play a key role in angiogenesis.

Tivozanib (AV-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R.

应 用

Tivozanib has been used in trials studying the treatment and basic science of Solid Tumors, Glioblastoma, Ovarian Cancer, Prostate Cancer, and Stage IV Disease, among others.

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