Tivozanib (AV-951)是一种有效的，选择性VEGFR抑制剂，作用于VEGFR1/2/3时，IC50分别为0.21 nM/0.16 nM/0.24 nM，也抑制PDGFR和c-Kit，作用于FGFR-1， Flt3， c-Met EGFR和IGF-1R活性较弱。AV-951 也抑制PDGFRß和c-Kit的磷酸化作用，IC50 分别为1.72nm 和1.63nM。AV-951阻断VEGF依赖的MAPK活性和内皮细胞增殖。AV-951是新型喹啉-尿素派生物。

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

替沃扎尼；AV-951；KRN951

DMSO ：16 mg/mL (35.2 mM)

VEGFR2 ,VEGFR3 ,EphB2 ,VEGFR1 ,PDGFRα

AV-951 is a novel quinoline-urea derivative. AV-951 blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells.

In vivo studies show that AV-951 also decreases the micro vessel density and suppresses VEGFR2 phosphorylation levels in tumor xenografts, especially at a concentration of 1mg/kg (p.o. administration). AV-951 shows almost complete inhibition of tumor xenografts growth (TGI>85%) in athymic rats. Another study in rat peritoneal disseminated tumor model shows that AV-951 could prolong the survival of the tumor-bearing rats with the MST of 53.5 days. AV-951 displays antitumor activity against many human tumor xenografts including lung, breast, colon, ovarian, pancreas and prostate cancer.

Antitumor activity and safety of tivozanib (AV-951) in a phase II randomized discontinuation trial in patients with renal cell carcinoma.
Nosovet al J Clin Oncol. 2012 May 10;30(14):1678-85. PMID: 