生物活性 | |||
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描述 | Survivin, a homodimeric member of the inhibitor of apoptosis protein (IAP) family, is required for cancer cell survival and overexpressed in almost all solid tumors. LQZ-7I is a survivin inhibitor. It has improved cytotoxicity with an IC50 of 3.1 µM against C4-2 cells and 4.8 µM against PC-3 cells. LQZ-7I significantly decreased the SEAP (secreted alkaline phosphatase) reporter expression. Furthermore, it significantly inhibited survivin dimerization. In C4-2 and PC-3 cells, LQZ-7I treatment reduced the expression of survivin in a time-dependent manner. Specifically, LQZ-7I treatment reduced the half-life of survivin from 2.2 and 2.3 hrs to 50 and 25 minutes in C4-2 and PC-3 cells, respectively. Moreover, LQZ-7I induced cleavage of caspase 3 in a dose dependent manner in both cell lines. 3 µM LQZ-7I induced ~48% and ~39% apoptosis in C4-2 and PC-3 cells, respectively. In vivo, LQZ-7I treatment at 100 mg/kg significantly suppressed tumor growth without any notable adverse effect on the mice as indicated by lacking changes in body weight[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.87mL 0.57mL 0.29mL |
14.35mL 2.87mL 1.44mL |
28.71mL 5.74mL 2.87mL |
参考文献 |
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