Tivozanib hydrochloride hydrate 是一种有效的、选择性的、具有口服活性的 VEGFR 酪氨酸激酶 抑制剂，对 VEGFR-1、VEGFR-2、VEGFR-3的 IC50 值分别为 0.21、0.16、0.24 nM。Tivozanib hydrochloride hydrate 抑制肿瘤组织中的血管生成和血管通透性，并显示出抗肿瘤活性。Tivozanib hydrochloride hydrate 具有研究转移性肾细胞癌 (RCC) 的潜力。
货号:ajcx38708
CAS:682745-41-1
分子式:C22H22Cl2N4O6
分子量：509.34
溶解度:DMSO : 250 mg/mL (490.83 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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

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].

[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.

Protocol:

VEGFR-1 0.21nM(IC50)

VEGFR-2 0.16nM(IC50)

VEGFR-3 0.24nM(IC50)