| 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 |
| 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： |
-80℃（运输条件：冰袋低温运输） |
| 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 |
|
| 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京