682745-41-1

682745-41-1 structure

682745-41-1 structure

Name: Tivozanib
Chemical Name: 1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea,hydrate,hydrochloride
CAS Number: 682745-41-1
Molecular Formula: C₂₂H₂₂Cl₂N₄O₆
Molecular Weight: 509.33900
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK VEGFR
Create Date: 2016-06-04 22:06:30
Modify Date: 2024-01-11 14:32:28

Name	1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea,hydrate,hydrochloride
Synonyms	Tivozanib hydrochloride monohydrate UNII-8A9H4VK35Z Tivozanib hydrochloride hydrate Tivozanib HCl hydrate Kil-8951 Tivozanib HCl

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.

Molecular Formula	C₂₂H₂₂Cl₂N₄O₆
Molecular Weight	509.33900
Exact Mass	508.09200
PSA	123.69000
LogP	5.81130
Storage condition	-20°C