米帕林盐酸盐

生物活性体外研究体内研究米帕林盐酸盐试剂级价格

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

米帕林盐酸盐化学性质

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)

安全信息

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)。

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.