米帕林盐酸盐
米帕林盐酸盐 性质
| 熔点 | 247 °C |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：10mg/mL（19.65mM）；； |
| 水溶解性 | 2.8 g/100 mL |
| CAS 数据库 | 6151-30-0(CAS DataBase Reference) |
米帕林盐酸盐 用途与合成方法
Quinacrine (5-20 μM; 24 hours) inhibits the growth of SGC-7901 cells.
Quinacrine (7.5 and 15 μM; 24 hours) induces apoptosis in SGC-7901 cells, which is associated with mitochondria-dependent signal pathway and involves p53 upregulation and caspase-3 activation pathway.
Quinacrine (15 μM; 24 hours) treatment significantly increased the levels of proapoptotic proteins, including cytochrome c, Bax, and p53, and decreased the levels of antiapoptotic protein Bcl-2, thus shifting the ratio of Bax/Bcl-2 in favor of apoptosis .
Cell Viability Assay
| Cell Line: | SGC-7901 cells |
| Concentration: | 0, 5, 10, 15, and 20 μM |
| Incubation Time: | 24 hours |
| Result: | Cell viability was inhibited in a dose-dependent manner, and the mean IC 50 value is 16.18 μM. |
Apoptosis Analysis
| Cell Line: | SGC-7901 cells |
| Concentration: | 7.5 and 15 μM |
| Incubation Time: | 24 hours |
| Result: | The percentage of apoptotic cells, including the early phase and late phase apoptosis, increased to 26.30%, compared with control group of 3.37%. |
Western Blot Analysis
| Cell Line: | SGC-7901 cells |
| Concentration: | 15 μM |
| Incubation Time: | 24 hours |
| Result: |
The relative quantity of cytochrome c protein was upregulated, increased from 0.10 to 0.24.
The relative quantity of p53 protein was dramatically increased, from 0.06 to 0.19. The Bax/Bcl-2 ratio was dramatically elevated from 1.21 to 2.59. |
Quinacrine (100 mg/kg three times per week for two consecutive weeks) significantly suppresses circulating blast cells at days 30/31 and increases the median survival time (MST). Quinacrine does not decrease the body weight of treated animals at the tested dose.
| Animal Model: | Female SCID mice with acute myeloid leukemia (AML)-PS model |
| Dosage: | 100 mg/kg |
| Administration: | Administered by oral gavage (po); three times a week for two consecutive weeks |
| Result: |
In the first AML mouse in vivo study, evaluation of circulating leukemic cells detected in blood samples (in percent of white blood cells (WBC)) at day 30/31 showed 72% human tumor cells in the control mice, whereas in mice treated with Quinacrine, this was only 2.2%.
The MST of control mice was 34 days whereas it was 46 days in Quinacrine-treated mice. |
