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CAS No.: 6975-75-3

ILK-IN-3 Catalog No. CSN27205

Synonyms: QLT-0267;QLT-267;NSC-21678

ILK-IN-3 is an integrin linked kinase inhibitor.

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技术信息

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 LCC6^Her2 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 LCC6^Her2 cells with ILK-IN-3 at a concentration of 10μM led to a ~79% and ~83% decrease in VEGF secretion, respectively. In MCF-7^Her2 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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.3059 mL
- 21.5293 mL
- 43.0586 mL
- 5 mM
- 0.8612 mL
- 4.3059 mL
- 8.6117 mL
- 10 mM
- 0.4306 mL
- 2.1529 mL
- 4.3059 mL

技术信息

CAS号

6975-75-3

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H12N6O

运输

蓝冰

分子量

232.24

别名

QLT-0267;QLT-267;NSC-21678

溶解度

DMSO	80.0 mg/mL (344.5 mM) warming

动物实验配方

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