Tivozanib hydrochloride hydrate(Synonyms: AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tivozanib hydrochloride hydrate (Synonyms: AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate) 纯度: 99.77%

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。

Tivozanib hydrochloride hydrate(Synonyms: AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate)

Tivozanib hydrochloride hydrate Chemical Structure

CAS No. : 682745-41-1

规格 价格 是否有货 数量
5 mg ￥790 In-stock
10 mg ￥1120 In-stock
50 mg ￥3170 In-stock
100 mg ￥5540 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

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].

IC50 & Target[3]

VEGFR-1

0.21 nM (IC50)

VEGFR-2

0.16 nM (IC50)

VEGFR-3

0.24 nM (IC50)

体外研究
(In Vitro)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

509.34

Formula

C22H22Cl2N4O6
CAS 号

682745-41-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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)
参考文献

  • [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.
Cell Assay

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [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.

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