Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations and also leads to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.
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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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 75629-57-1 |
分子式 | C16H12ClNO |
分子量 | 269.726 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(389.28 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |