二盐酸奎吖因水合物
| 中文名称 | 二盐酸奎吖因水合物 |
|---|---|
| 中文同义词 | 疟疾平;二盐酸喹吖因;喹吖因二盐酸;阿的平 二盐酸盐;二盐酸阿的平;二盐酸喹丫因;疟涤平;盐酸阿的平 |
| 英文名称 | QUINACRINE DIHYDROCHLORIDE |
| 英文同义词 | 6-CHLORO-9-(4-DIETHYLAMINO-1-METHYL-BUTYLAMINO)-2-METHOXYACRIDINE DIHYDROCHLORIDE;6-CHLORO-9-(4-DIETHYLAMINO-1-METHYL-N-BUTYL)AMINO-2-METHOXYACRIDINE DIHYDROCHLORIDE;ERION HYDROCHLORIDE;DL-QUINACRINE HYDROCHLORIDE;CHINACRIN HYDROCHLORIDE;CHEMIOCHIN HYDROCHLORIDE;ARICHIN HYDROCHLORIDE;ATABRINE HYDROCHLORIDE |
| CAS号 | 69-05-6 |
| 分子式 | C23H32Cl3N3O |
| 分子量 | 472.88 |
| EINECS号 | 200-700-8 |
| 相关类别 | 小分子抑制剂;细胞信号和神经生物学;细胞生物学 |
| Mol文件 | 69-05-6.mol |
| 结构式 |  |
二盐酸奎吖因水合物 性质
| 熔点 | 249-251℃ (Decomposition) |
|---|---|
| 密度 | 1.2962 (rough estimate) |
| 折射率 | 1.6300 (estimate) |
| 储存条件 | +15C to +30C |
| 溶解度 | 可溶于DMSO（轻微）、甲醇（轻微、超声处理）、水（轻微） |
| 形态 | 黄色固体 |
| 酸度系数(pKa) | pKa -6.3(H2O t undefined I not reported but low) (Uncertain) |
| 颜色 | 浅黄色至厚黄色 |
| PH值 | 3.0～5.0 (20g/l, 25℃) |
| 水溶解性 | Water: 33.33 mg/mL (70.48 mM) |
| Merck | 14,8044 |
| BRN | 4834013 |
| 稳定性 | 稳定的。与强氧化剂不相容。 |
| EPA化学物质信息 | Quinacrine hydrochloride (69-05-6) |
| Target | Value |
|
PLA2
() |
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. |
安全信息
| 危险品标志 | Xn |
|---|---|
| 危险类别码 | 22-36/37/38 |
| 安全说明 | 36/37/39 |
| WGK Germany | 3 |
| RTECS号 | AR7875000 |
| 毒性 | LD50 oral in rabbit: 433mg/kg |