Tivozanib (AV-951) (C09-1073-990)

InformationTivozanib (AV-951, KRN-951) is a potent and selectiveVEGFRinhibitor forVEGFR1/2/3with 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. Phase 3.In vitroAV-951 is a novel quinoline-urea derivative. AV-951 blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells.In vivoIn 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.Cell Datacell lines：Concentrations：1 μMIncubation Time：15 minutesPowder Purity:≥95%. Specifications and Purity: 10mM in DMSO. Molecular Formula: C22H19ClN4O5. Molecular Weight: 454.86.