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Tivozanib

Names

[ CAS No. ]:
682745-41-1

[ Name ]:
Tivozanib

[Synonym ]:
Tivozanib hydrochloride monohydrate
UNII-8A9H4VK35Z
Tivozanib hydrochloride hydrate
Tivozanib HCl hydrate
Kil-8951
Tivozanib HCl

Biological Activity

[Description]:

Tivozanib hydrochloride hydrate is a potent and selective and orally active VEGFR tyrosine kinase inhibitor with IC50是of 0.21, 0.16, 0.24 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively. Tivozanib hydrochloride hydrate inhibits angiogenesis and vascular permeability in tumor tissues and shows antitumor activity. Tivozanib hydrochloride hydrate has the potential for the research of metastatic renal cell carcinoma (RCC) [1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

[Target]

VEGFR-1:0.21 nM (IC50)

VEGFR-2:0.16 nM (IC50)

VEGFR-3:0.24 nM (IC50)


[In Vitro]

Tivozanib hydrochloride hydrate inhibits the phosphorylation of VEGFR-1, VEGFR-2 and VEGFR-3[2].

[In Vivo]

Tivozanib hydrochloride hydrate (1 mg/kg; p.o.; 14 days) suppresses the development of CNV lesions and leds to a significant regression of established CNV, reducing the affected areas by 67.7%[4].

[References]

[1]. Motzer RJ, et al. Tivozanib versus sorafenib as initial targeted therapy for patients with metastatic renal cell carcinoma: results from a phase III trial. J Clin Oncol. 2013 Oct 20;31(30):3791-9.

[2]. De Luca A, et al. Tivozanib, a pan-VEGFR tyrosine kinase inhibitor for the potential treatment of solid tumors. IDrugs. 2010 Sep;13(9):636-45.

[3]. Eskens FA, det al. Biologic and clinical activity of tivozanib (AV-951, KRN-951), a selective inhibitor of VEGF receptor-1, -2, and -3 tyrosine kinases, in a 4-week-on, 2-week-off schedule in patients with advanced solid tumors. Clin Cancer Res. 2011 Nov 15;17(22):7156-63.

[4]. Kang S, et al. Antiangiogenic effects of tivozanib, an oral VEGF receptor tyrosine kinase inhibitor, on experimental choroidal neovascularization in mice. Exp Eye Res. 2013 Jul;112:125-33.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H22Cl2N4O6

[ Molecular Weight ]:
509.33900

[ Exact Mass ]:
508.09200

[ PSA ]:
123.69000

[ LogP ]:
5.81130

[ Storage condition ]:
-20°C

Related Compounds