生物活性 | |||
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描述 | Survivin plays a pivotal role in not only cell survival but also cell cycle progression. Op18 (stathmin) is an oncoprotein that regulates microtubule stabilization. Both survivin and Op18 have been proposed as therapeutic targets for cancer. GDP366, a novel small molecule dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells. HCT116 cells were exposed to escalating concentrations of GDP366 for 48 hours or a fixed concentration (2.0 μM) of GDP366 for various durations, western blotting analysis revealed a dose- and time-dependent decrease of survivin and Op18, while the expression of p53 and p21 was remarkably increased in a dose- and time-dependent manner. Moreover, GDP366 inhibited the surviving clonogenic HCT116 cells in a dose-dependent manner, with an IC50 value of approximately 1.0 μM. In BALB/c mice inoculated with HCT116 cells, GDP366 at the dosage of 50 mg/kg, daily i.p., for 16 d potently inhibited the growth of HCT116 tumors. GDP366-treated tumors were significantly lower in weight than control tumors[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.66mL 0.53mL 0.27mL |
13.32mL 2.66mL 1.33mL |
26.63mL 5.33mL 2.66mL |
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