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ILK-IN-3

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Chemical Structure| 6975-75-3 同义名 : -
CAS号 : 6975-75-3
货号 : A1327308
分子式 : C10H12N6O
纯度 : 99%+
分子量 : 232.242
MDL号 : MFCD01239326
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(366 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：
生物活性
描述 The integrin-linked kinase (ILK) is an intracellular serine/threonine kinase highly expressed in normal pancreatic, cardiac and skeletal muscle tissues. It plays an essential role in integrin and growth factor receptor-related signaling pathways. Targeted inhibition of ILK in cancer cells may reduce tumor growth. ILK-IN-3 (also known as QLT0267) is a small-molecule ILK inhibitor. The ED values of ILK-IN-3 for the inhibition of the viability of human breast tumor cell lines were 9.8 - 55.8μM. In both LCC6 and LCC6Her2 cells, treatment with ILK-IN-3 (0.3 - 42.67μM) alone or in combination with docetaxel reduced P-AKT (Ser473) levels in a dose-dependent manner. Treatment of LCC6 and LCC6Her2 cells with ILK-IN-3 at a concentration of 10μM led to a ~79% and ~83% decrease in VEGF secretion, respectively. In MCF-7Her2 cells, combined treatment with ILK-IN-3 (10μM) and docetaxel (0.25 nM) for 72 hours significantly reduced VEGF secretion compared with the control group. The combined therapy of ILK-IN-3 (200mg/kg, oral administration) and docetaxel (5mg/kg, intravenous administration) for 4 weeks reduced tumor burden and extended survival in mice implanted orthotopically with LCC6 breast cancer cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.31mL

0.86mL

0.43mL

21.53mL

4.31mL

2.15mL

43.06mL

8.61mL

4.31mL
参考文献

[1]Kalra J, Anantha M, Warburton C, et al. Validating the use of a luciferase labeled breast cancer cell line, MDA435LCC6, as a means to monitor tumor progression and to assess the therapeutic activity of an established anticancer drug, docetaxel (Dt) alone or in combination with the ILK inhibitor, QLT0267. Cancer Biol Ther. 2011;11(9):826-838. doi:10.4161/cbt.11.9.15183

[2]Kalra J, Warburton C, Fang K, Edwards L, Daynard T, Waterhouse D, Dragowska W, Sutherland BW, Dedhar S, Gelmon K, Bally M. QLT0267, a small molecule inhibitor targeting integrin-linked kinase (ILK), and docetaxel can combine to produce synergistic interactions linked to enhanced cytotoxicity, reductions in P-AKT levels, altered F-actin architecture and improved treatment outcomes in an orthotopic breast cancer model. Breast Cancer Res. 2009;11(3):R25