• 产品描述： OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner[2]. OSU-T315 causes cell death through apoptosis and autophagy

• 靶点： IC50: 0.6μM; Integrin-linked kinase (ILK) inhibitor;Apoptosis; Integrin; Autophagy

• 体外研究：
  OSU-T315 (Compound 22; 0-5 μM; 24 hours) exhibits high in vitro potency against a panel of prostate and breast cancer cell lines with a IC50 range of 1-2.5 μM. OSU-T315 (0-2.5 μM; 24 hours) can reduce YB-1, HER2, and EGFR expression; shows a modest suppressive effect on phosphorylated S6 levels, exhibits dose-dependent suppressive effects on the levels of phospho-ERK1/2 and phospho-p38, while that of phospho-JNK remains unaltered in PC-3 cell. OSU-T315 (0-4 μM; 24 hours) causes autophagy through ILK inhibition. Western Blot Analysis Cell Line: PC-3 cells; MDA-MB-231 cells Concentration: 1 μM, 2 μM, 3 μM, 4 μM; 0.5 μM, 1 μM, 1.5 μM, 2 μM, 2.5 μM Incubation Time: 24 hours Result: Exhibited a dose-dependent decreasing effect on the phosphorylation of pS6, ERKs, and p38 in PC-3 cells and MDA-MB-231 cells. Cell Viability Assay Cell Line: Prostate cancer cells: LNCaP, PC-3; breast cancer cells: MDA-MB-231, MDA-MB-468, SKBR3, MCF-7; PrEC and MEC cells Concentration: 0-5 μM Incubation Time: 24 hours Result: Suppressed cancer cells viability in breast and prostate cancer cells (IC (50), 1-2.5μM). Apoptosis Analysis Cell Line: PC-3 cells Concentration: 1 μM, 2 μM, 3 μM, 4 μM Incubation Time: 24 hours Result: Induced accumulation of LC3-II and PARP cleavage

• 体内研究：
  OSU-T315 (Oral gavage; 25 mg/kg, 50 mg/kg; single daily; 35 days) has a suppressive effect of on PC-3 xenograft tumor growth . No other obvious toxicity is observed in mice. Animal Model: Male NCr athymic nude mice with PC-3 tumor xenografts Dosage: 25 mg/kg; 50 mg/kg Administration: Oral gavage; single daily; 35 days Result: Resulted in suppression of tumor growth relative to the vehicle control after 35 days of treatment (48% and 62% suppression for 25 and 50 mg/kg, respectively).

• 参考文献：
  1. Su-Lin Lee,et al Identification and Characterization of a Novel Integrin-Linked Kinase Inhibitor.J Med Chem. 2011 Sep 22; 54(18): 6364–6374 2. Liu TM, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95. [

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.874 ml	9.37 ml	18.741 ml
  5 mM	0.375 ml	1.874 ml	3.748 ml
  10 mM	0.187 ml	0.937 ml	1.874 ml
  50 mM	0.037 ml	0.187 ml	0.375 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *