| 產(chǎn)品描述： | OSU-T315 is a novel potent, orally active ILK (integrin-linked kinase) inhibitor with IC50 of 0.6 μM. |
| 靶點(diǎn)： |
Integrin |
| 體外研究： |
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 |
| 體內(nèi)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) |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京