产品说明书

Ki8751

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Chemical Structure| 228559-41-9 同义名 : -
CAS号 : 228559-41-9
货号 : A187238
分子式 : C24H18F3N3O4
纯度 : 98+%
分子量 : 469.413
MDL号 : MFCD09971092
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: 35 mg/mL(74.56 mM)，配合低频超声，并水浴加热至45℃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：

IP 2% DMSO+2% Tween80+30% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 42 mg/mL suspension

生物活性
靶点

  • VEGFR2

    VEGFR2, IC50:0.9 nM

  • PDGFRα

    PDGFRα, IC50:67 nM

  • c-Kit

    c-Kit, IC50:40 nM
描述 Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, which is > 40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.07mL

21.30mL

4.26mL

2.13mL
参考文献

[1]Tamura D, Arao T, et al. Bortezomib potentially inhibits cellular growth of vascular endothelial cells through suppression of G2/M transition. Cancer Sci. 2010 Jun;101(6):1403-8.

[2]Kubo K, Shimizu T, et al. Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas. J Med Chem. 2005 Mar 10;48(5):1359-66.