二盐酸奎吖因水合物
- CAS号:69-05-6
- 英文名:QUINACRINE DIHYDROCHLORIDE
- 中文名:二盐酸奎吖因水合物
- CBNumber:CB8320579
- 分子式:C23H32Cl3N3O
- 分子量:472.88
- MOL File:69-05-6.mol
- 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 :DMSO (Slightly), Methanol (Slightly, Sonicated), Water (Slightly)
- 形态 :Yellow solid
- 酸度系数(pKa) :pKa -6.3(H2O t undefined I not reported but low) (Uncertain)
- 颜色 :Light Yellow to Yellow
- 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 :Stable. Incompatible with strong oxidizing agents.
- EPA化学物质信息 :Quinacrine hydrochloride (69-05-6)
- 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
二盐酸奎吖因水合物性质、用途与生产工艺
- 生物活性 Quinacrine 2HCl是具有多种作用的亲脂性阳离子药物，通常用作抗原生动物剂。Quinacrine是有效的phospholipase A2抑制剂。
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靶点
Target Value PLA2
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体外研究
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. -
体内研究
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. - 类别 有毒物质
- 毒性分级 中毒
- 急性毒性 口服- 大鼠 LD50: 660 毫克/ 公斤; 口服- 小鼠 LD50: 557 毫克/ 公斤
- 可燃性危险特性 可燃;火场释放有毒氮氧化物, 氯化物烟雾
- 储运特性 库房低温, 通风, 干燥
- 灭火剂 水, 二氧化碳, 泡沫, 沙土
- 更新日期：2024/04/30
- 产品编号：HY-13735A
- 产品名称：二盐酸奎吖因水合物 Quinacrine dihydrochloride
- CAS编号：69-05-6
- 包装：100mg
- 价格：496元
- 更新日期：2024/04/30
- 产品编号：S4255
- 产品名称：疟疾平 Quinacrine 2HCl
- CAS编号：69-05-6
- 包装：50mg
- 价格：800.64元
- 公司名称：ARONIS
- 联系电话：--
- 电子邮件：aronis@aronis.ru
- 国家：俄罗斯
- 产品数：6593
- 优势度：60
