米帕林盐酸盐
- CAS号:6151-30-0
- 英文名:Mepacrine hydrochloride
- 中文名:米帕林盐酸盐
- CBNumber:CB4138653
- 分子式:C23H36Cl3N3O3
- 分子量:508.91
- MOL File:6151-30-0.mol
- 熔点 :247 °C
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: 10 mg/mL (19.65 mM);;
- 水溶解性 :2.8 g/100 mL
- CAS 数据库 :6151-30-0(CAS DataBase Reference)
- 危险品标志 :Xn
- 危险类别码 :22-36/37/38
- 安全说明 :26-37/39
米帕林盐酸盐性质、用途与生产工艺
- 生物活性 Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) 是一种抗疟剂 (antimalarial)，在体内外均具有抗肿瘤作用。Quinacrine hydrochloride hydrate 抑制 NF-κB 并激活 p53 信号转导，诱导肿瘤细胞发生凋亡 (apoptosis)。
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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.
- 更新日期：2024/11/08
- 产品编号：S5435
- 产品名称：米帕林盐酸盐 Quinacrine Dihydrochloride Dihydrate
- CAS编号：6151-30-0
- 包装：25mg
- 价格：794.67元
- 公司名称：Whyte Chemicals
- 联系电话：--
- 电子邮件：sales@whytechemicals.co.uk
- 国家：英国
- 产品数：3748
- 优势度：50
