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OSU-T315 99%

OSU-T315

源葉(MedMol)
S82868
1333146-24-9
C30H30F3N5O
533.5873
品牌 貨號 產品規格 價格(RMB) 庫存(上海) 北京 武漢 南京 購買數量
源葉(MedMol) S82868-1mg 99% ¥400.00元 10 - - -
源葉(MedMol) S82868-2mg 99% ¥650.00元 10 - - -
源葉(MedMol) S82868-5mg 99% ¥1000.00元 >10 - - -
源葉(MedMol) S82868-10mg 99% ¥1300.00元 >10 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

OSU-T315 is a novel potent, orally active ILK (integrin-linked kinase) inhibitor with IC50 of 0.6 μM.
產品描述: OSU-T315 is a novel potent, orally active ILK (integrin-linked kinase) inhibitor with IC50 of 0.6 μM.
靶點: 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:
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
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參考文獻

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