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Tivozanib

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Chemical Structure| 475108-18-0 同义名 : KRN951;AV-951;KRN-951, Tivozanib
CAS号 : 475108-18-0
货号 : A770204
分子式 : C22H19ClN4O5
纯度 : 99%+
分子量 : 454.86
MDL号 : MFCD15146788
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(54.96 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300+water 1 mg/mL

生物活性
靶点

  • VEGFR1

    VEGFR1, IC50:30 nM

  • VEGFR3

    VEGFR3, IC50:15 nM

  • VEGFR2

    VEGFR2, IC50:6.5 nM

  • PDGFRβ

    PDGFRβ, IC50:49 nM
描述 Tivozanib is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
MCF7 cells Proliferation assay Antiproliferative activity against human MCF7 cells, IC50=0.38 μM 24583357
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03419572 - Recruiting January 5, 2021 -
NCT00970411 Solid Tumors Phase 1 Completed - Japan ... 展开 >> Shizuoka, Japan 收起 <<
NCT01058655 Gastrointestinal Cancer Phase 1 Phase 2 Completed - United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02115 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

10.99mL

2.20mL

1.10mL

21.98mL

4.40mL

2.20mL
参考文献

[1]Taguchi E, Nakamura K, et al. Anti-tumor activity and tumor vessel normalization by the vascular endothelial growth factor receptor tyrosine kinase inhibitor KRN951 in a rat peritoneal disseminated tumor model. Cancer Sci. 2008 Mar;99(3):623-30.

[2]Nakamura K, Taguchi E, et al. KRN951, a highly potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, has antitumor activities and affects functional vascular properties. Cancer Res. 2006 Sep 15;66(18):9134-42.