• 产品描述： OSU-T315 is a novel potent, orally active ILK (integrin-linked kinase) inhibitor with IC50 of 0.6 μM.

• 靶点： Integrin

• 体外研究：
  OSU-T315 exhibited high in vitro potency against a panel of prostate and breast cancer cell lines (IC(50), 1-2.5 μM), while normal epithelial cells were unaffected. OSU-T315 facilitated the dephosphorylation of Akt at Ser-473 and other ILK targets, including glycogen synthase kinase-3β and myosin light chain. Moreover, OSU-T315 suppressed the expression of the transcription/translation factor YB-1 and its targets HER2 and EGFR in PC-3 cells, which could be rescued by the stable expression of constitutively active ILK. The cytotoxicity of OSU-T315 in normal B or T cells was significantly lower (LC50 > 10 μM). OSU-T315 had the effect of dose-dependent cytotoxicity toward 2 CLL-derived cell lines, Mec-1 and OSU-CLL (LC50 of 2-3 μM in both) after 24-hour treatment

• 体内研究：
  Athymic nude mice bearing established subcutaneous PC-3 tumors were treated with oral OSU-T315 once daily at 25 and 50 mg/kg or vehicle control. The daily administration of OSU-T315 at both doses was well tolerated. Treatment with oral OSU-T315 in either dose resulted in significant 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. 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. 2. Lee SL, et al. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.874 ml	9.371 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

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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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 *