生物活性 | |||
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描述 | The oncogenic gene K-Ras mutations are frequently found in various cancers and are associated with resistance to treatment or poor prognosis. Oncrasin-1 is a potent and effective anticancer inhibitor against various lung cancer cells with K-Ras mutations at low or submicromolar concentrations. Oncrasin-1 induced dose-dependent cytotoxicity in T29Kt1 cells with an IC50 of 4.81 μM. Oncrasin-1 effectively killed K-Ras–mutant H460, H2122, H2887, and A549 cells with an IC50 of ≤3 μM. Oncrasin-1 (10 μM) effectively induced cell killing in T29Kt1 and H460 cells. Additionally, treatment of H460 cells with 1 μM oncrasin-1 effectively activated caspases 3 and 8. Oncrasin-1 (100 mg/kg/injection daily for 10 days) suppressed tumor growth by 75.4% in mice. Treatment with oncrasin-1 also prolonged survival: the mean survival times for mice treated with solvent and oncrasin-1 were 24 and 32, respectively, demonstrating that Oncrasin-1 might be useful for the treatment of cancers with K-Ras mutations[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.71mL 0.74mL 0.37mL |
18.54mL 3.71mL 1.85mL |
37.07mL 7.41mL 3.71mL |
参考文献 |
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