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MedChemExpress - Model Tivozanib hydrochloride hydrate - 682745-41-1

Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy[1].

Tivozanib hydrochloride hydrate

MCE China：Tivozanib hydrochloride hydrate

Brand：MedChemExpress (MCE)

Cat. No.HY-10977A

CAS：682745-41-1

Synonyms：AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate

Purity：99.77%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy.

In Vitro：Tivozanib hydrochloride hydrate inhibits the phosphorylation of VEGFR-1, VEGFR-2, and VEGFR-3, with IC50s of 0.16-0.24 nM[1].Tivozanib hydrochloride hydrate (0-100 nM, 24 h) inhibits VEGF-induced proliferation of HUVECs with IC50 of 0.67 nM, and migration of HUVECs in dose-dependent manner[1]. Tivozanib hydrochloride hydrate (0-300 nM, 1 h) selectively inhibits the VEGF-stimulated phosphorylation of MAPKs in endothelial cells ligand-dependently, with IC50s of 0.13 and 0.18 nM for ERK1 and ERK2, respectively[1].

In Vivo：Tivozanib hydrochloride hydrate (0.04-1 mg/kg, po for 14 days) exhibits antitumor efficacy against breast, colon, hepatic, lung, ovarian, pancreatic, and prostate cancer in athymic mice model[1].Tivozanib hydrochloride hydrate (0.2-1 mg/kg, po for 21 days) reversibly suppresses vascular permeability and angiogenesis in Calu-6 tumor bearing rats model[1].Tivozanib hydrochloride hydrate (5 mg/kg, po, single dose) reveals a AUCinf of 44.5 μg·h/mL, Cmax of 2823 ng/mL in athymic mice model[1].

IC50 & Target：VEGFR-2 6.5 nM (IC50) VEGFR-3 15 nM (IC50) VEGFR-1 30 nM (IC50)

References：

[1]. Nakamura K, et al., KRN951, a highly potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, has antitumor activities and affects functional vascular properties. Cancer Res. 2006 Sep 15;66(18):9134-42. [Content Brief]

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