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N-[2-氯-4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基]-N'-(5-甲基-3-异恶唑基)脲

用途

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].
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名称

[ CAS 号 ]:
682745-41-1

[ 中文名 ]:
N-[2-氯-4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基]-N'-(5-甲基-3-异恶唑基)脲

[ 英文名 ]:
Tivozanib

[英文别名 ]:

生物活性

[ 描述 ]:

盐酸替沃扎尼水合物是一种有效、选择性和口服活性VEGFR酪氨酸激酶抑制剂,具有IC50是分别为0.21、0.16、0.24 nM。盐酸替沃扎尼水合物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。盐酸替沃扎尼水合物具有研究转移性肾细胞癌的潜力[1][2][3]。

[ 相关类别 ]:

研究领域 >> 癌症
信号通路 >> 蛋白酪氨酸激酶 >> VEGFR

[ 靶点 ]

VEGFR-1:0.21 nM (IC50)

VEGFR-2:0.16 nM (IC50)

VEGFR-3:0.24 nM (IC50)


[体外研究]

盐酸替沃扎尼水合物抑制VEGFR-1、VEGFR-2和VEGFR-3的磷酸化[2]。

[体内研究]

盐酸替沃扎尼水合物(1 mg/kg；p.o.；14天)抑制CNV病变的发展,并导致已建立的CNV显著消退,使受影响区域减少67.7%[4]。

[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.

物理化学性质

[ 分子式 ]:
C22H22Cl2N4O6

[ 分子量 ]:
509.33900

[ 精确质量 ]:
508.09200

[ PSA ]:
123.69000

[ LogP ]:
5.81130

[ 储存条件 ]:
-20°C

推荐生产厂家/供应商：

公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

价格：

联系人：徐经理

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相关化合物

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标题：682745-41-1_CAS号:682745-41-1_N-[2-氯-4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基]-N'-(5-甲基-3-异恶唑基)脲 - 化源网 地址：https://m.chemsrc.com/mip/cas/682745-41-1_984950.html