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ILK-IN-2

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Chemical Structure| 1333146-24-9 同义名 : OSU-T315 analog;CPD 22;OSU-T315 (1,5-regioisomer);T315(1,5);ILK inhibitor 22(1,5);OSU-T 315;Integrin-linked Kinase Inhibitor 1
CAS号 : 1333146-24-9
货号 : A814222
分子式 : C30H30F3N5O
纯度 : 99%+
分子量 : 533.587
MDL号 : MFCD29472239
存储条件:

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

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(93.71 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 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.87mL

0.37mL

0.19mL

9.37mL

1.87mL

0.94mL

18.74mL

3.75mL

1.87mL

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.