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CAS No.: 1333146-24-9

ILK-IN-2 Catalog No. CSN17699

Synonyms: OSU-T315 analog;OSU-T 315;CPD 22

ILK-IN-1 is an ILK inhibitor with IC50 of 0.6 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述OSU-T315 is a novel ILK inhibitor with IC50 value of 0.6μM. OSU-T315 at concentration<5μM dose-dependently inhibited the proliferation of PC-3 and LNCaP prostate cancer cells and MDA-MB-231, MDA-MB-468, SKBR3, and MCF-7 breast cancer cells in 5% FBS-supplemented medium after 24 h of treatment. Through inhibition of ILK, OSU-T315 facilitated the dephosphorylation of Akt at Ser-473 and other ILK targets, including GSK-3β and myosin light chain. Further study showed that it suppressed the expression of the transcription/translation factor YB-1 and its targets HER2 and EGFR in PC-3 cells in 5% FBS-supplemented medium, which could be rescued by the stable expression of constitutively active ILK. It induced autophagy at 1μM and apoptosis at 4μM, both of which were integral to its antiproliferative activity. Oral administration of OSU-T315 at dose of 25mg/kg or 50mg/kg once daily for 35 days reduced tumor growth of athymic nude mice xenograft PC-3 cells^[2].
参考文献

[1] Lee SL, Hsu EC, et al. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74.
[2] Lee SL, Hsu EC, Chou CC, Chuang HC, Bai LY, Kulp SK, Chen CS. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74. doi: 10.1021/jm2007744. Epub 2011 Aug 24. PMID: 21823616; PMCID: PMC3182772.

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
- 1.8741 mL
- 9.3705 mL
- 18.7411 mL
- 5 mM
- 0.3748 mL
- 1.8741 mL
- 3.7482 mL
- 10 mM
- 0.1874 mL
- 0.9371 mL
- 1.8741 mL

技术信息

CAS号

1333146-24-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H30F3N5O

运输

蓝冰

分子量

533.59

别名

OSU-T315 analog;OSU-T 315;CPD 22;Integrin-linked Kinase Inhibitor 1;ILK inhibitor 22(1,5);T315(1,5);OSU-T315 (1,5-regioisomer)

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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