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6151-30-0

中文名称 米帕林盐酸盐
英文名称 Mepacrine hydrochloride
CAS 6151-30-0
分子式 C23H36Cl3N3O3
MDL 编号 MFCD00150069
分子量 508.91
MOL 文件 6151-30-0.mol
更新日期 2023/03/24 18:27:27
6151-30-0 结构式 6151-30-0 结构式

基本信息

中文别名
米帕林
盐酸阿伯平
N4-(6-氯-2-甲氧基-9-吖啶基)-N1,N1-二乙基-1,4-戊二胺二盐酸盐二水合物
奎纳克林盐酸盐
米帕林盐酸盐
英文别名
QUINACRINE DIHYDROCHLORIDE DIHYDRATE
QUINACRINE HYDROCHLORIDE, DIHYDRATE
6-chloro-9-((4-(diethylamino)-1-methylbutyl)amino)-2-methoxy-acridindihydr
6-chloro-9-((4-(diethylamino)-1-methylbutyl)amino)-2-methoxyacridinedihydroc
atabrinehydrochloridedihydrate
hloride2h2-o
mepacrinehcl
mepacrinehydrochloridedihydrate
ochloride,dihydrate
AtabrineMepacnine
QuinacrineHCl
Quinacrinehydrochlorid
QUINACRINE,ATABRINE MEPACNINE
Mepacrine hydrochloride
N4-(6-Chloro-2-methoxy-9-acridinyl)-N1,N1-diethyl-1,4-pentanediamine dihydrochloride dihydrate
所属类别
原料药:抗疟药

物理化学性质

熔点247 °C
储存条件-20°C储存
溶解度DMSO: 10 mg/mL (19.65 mM);;
水溶解性2.8 g/100 mL

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H315-H319-H335
危险品标志Xn
危险类别码R22-R36/37/38
安全说明S26-S37/39
米帕林盐酸盐价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/01/16S5435米帕林盐酸盐
Quinacrine Dihydrochloride Dihydrate
6151-30-025mg794.67元

常见问题列表

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)。
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.
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