产品说明书
Quinacrine dihydrochloride
 |
同义名 : | 喹吖因 二盐酸盐 ;Mepacrine dihydrochloride;SN-390 dihydrochloride;Quinacrine 2HCl |
| CAS号 : | 69-05-6 | |
| 货号 : | A266175 | |
| 分子式 : | C23H32Cl3N3O | |
| 纯度 : | 98% | |
| 分子量 : | 472.88 | |
| MDL号 : | MFCD00012659 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
H2O: 12 mg/mL(25.38 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Quinacrine dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. 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[3]. The in vivo use of quinacrine (100mg/kg three times per week for two consecutive weeks) significantly suppressed circulating blast cells at days 30/31 and increased the median survival time (MST). The in vitro drug combination analysis yielded promising synergistic interactions when combining quinacrine with cytarabine, azacitidine and geldanamycin[4]. Quinacrine 25 mg/kg was shown to protect 70% of mice (statistically significant) from a lethal challenge with mouse-adapted EBOV (Ebola virus) with once-daily intraperitoneal dosing for 8 days[5]. QA (Quinacrine) demonstrates high degree of cytotoxicity against both immortalized and primary patient-derived cell lines with sub-micromolar 50% inhibitory concentration (IC50) values ranging from 1.2 µM (H2452) to 5.03 µM (H28). Further, QA also inhibited cellular migration and colony formation in MPM cells, demonstrated using scratch and clonogenic assays, respectively[6]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00574483 | Renal Cell Carcinoma | Phase 2 | Withdrawn(reevaluation of comp... 展开 >>ound development) 收起 << | January 2008 | United States, New York ... 展开 >> Community Care Physicians Albany, New York, United States, 12208 United States, North Carolina ClinWorks Cancer Research Center Charlotte, North Carolina, United States, 28207 收起 << |
| NCT00183092 | - | Completed | - | - | |
| NCT00183092 | Creutzfeldt-Jakob Disease | Phase 2 | Completed | - | United States, California ... 展开 >> University of California, San Francisco San Francisco, California, United States, 94143 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.11mL 0.42mL 0.21mL |
10.57mL 2.11mL 1.06mL |
21.15mL 4.23mL 2.11mL |
| 参考文献 |
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