Tivozanib, Free Base **

产品名称：Tivozanib, Free Base
产品货号：LC  T-6466
产品规格：1 G
Tivozanib, also known as AV-951, is a VEGF receptor tyrosine kinase inhibitor.
Tivozanib strongly inhibited VEGFR-1, VEGFR-2, and VEGFR-3 tyrosine kinases with IC50 values of 30, 6.5, and 15 nM, respectively.  It also inhibited EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie2 tyrosine kinases with IC50 values of 24, 40, 49, 78, and 78 nM, respectively.  Furthermore, it inhibited several other tyrosine kinases with IC50 values greater than for VEGFR-2.  Tivozanib markedly inhibited the ligand-induced phosphorylation of VEGFR-1, VEGFR-2, and VEGFR-3 in cellular assays, with IC50 values of 0.21, 0.16, and 0.24 nM, respectively.  It strongly inhibited VEGF-dependent phosphorylation of MAPKs in HUVECs, with IC50 values of 0.13 and 0.18 nM for extracellular signal-regulated kinase 1 (ERK1) and ERK2, respectively.  It also inhibited the VEGF-induced proliferation of HUVECs with an IC50 of 0.67 nM.  Tivozanib inhibited tumor growth in vivo in athymic rat xenograft models of breast, colon, hepatic, lung, ovarian, pancreatic, and prostate tumors.  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. 66:  9134-9142 (2006).
A phase II clinical trial demonstrated an overall response rate of 25% and a median progression-free survival time of 11.8 months in patients with advanced renal cell carcinoma treated with tivozanib as a single agent.  Hypertension and dysphonia were the most frequent side effects.  De Luca, A. and Normanno, N.  "Tivozanib, a pan-VEGFR tyrosine kinase inhibitor for the potential treatment of solid tumors."  IDrugs 13:  636-645 (2010).
Related CAS numbers:  682745-41-1 for the tivozanib monohydrochloride monohydrate.
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 5 mg/mL with warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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