Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib. It is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2, and 3, with IC50s of 30, 6.5, and 15 nM, respectively. It demonstrates antitumor efficacy.
- Selective, orally active inhibitor for VEGFR-1, 2, and 3
- Exhibits antitumor efficacy
- Inhibits phosphorylation of VEGFR-1, VEGFR-2, and VEGFR-3 with IC50s of 0.16-0.24 nM in vitro
- Inhibits VEGF-induced proliferation and migration of HUVECs in vitro
- Selectively inhibits VEGF-stimulated phosphorylation of MAPKs in endothelial cells in vitro
- Shows antitumor efficacy against breast, colon, hepatic, lung, ovarian, pancreatic, and prostate cancer in athymic mice models in vivo
- Reversibly suppresses vascular permeability and angiogenesis in Calu-6 tumor bearing rats in vivo