生物活性 | |||
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描述 | OSU-T315 is a novel ILK inhibitor with IC50 value of 0.6μM. OSU-T315 at concentration<5μM dose-dependently inhibited the proliferation of PC-3 and LNCaP prostate cancer cells and MDA-MB-231, MDA-MB-468, SKBR3, and MCF-7 breast cancer cells in 5% FBS-supplemented medium after 24 h of treatment. Through inhibition of ILK, OSU-T315 facilitated the dephosphorylation of Akt at Ser-473 and other ILK targets, including GSK-3β and myosin light chain. Further study showed that it suppressed the expression of the transcription/translation factor YB-1 and its targets HER2 and EGFR in PC-3 cells in 5% FBS-supplemented medium, which could be rescued by the stable expression of constitutively active ILK. It induced autophagy at 1μM and apoptosis at 4μM, both of which were integral to its antiproliferative activity. Oral administration of OSU-T315 at dose of 25mg/kg or 50mg/kg once daily for 35 days reduced tumor growth of athymic nude mice xenograft PC-3 cells[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.87mL 0.37mL 0.19mL |
9.37mL 1.87mL 0.94mL |
18.74mL 3.75mL 1.87mL |
参考文献 |
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