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69-05-6

中文名称 疟疾平
英文名称 QUINACRINE DIHYDROCHLORIDE
CAS 69-05-6
分子式 C23H32Cl3N3O
分子量 472.88
MOL 文件 69-05-6.mol
更新日期 2024/07/29 09:30:22
69-05-6 结构式 69-05-6 结构式

基本信息

中文别名
阿得平
疟涤平
疟疾平
奎克林
奎納克林
盐酸米帕林
盐酸阿的平
喹吖因二盐酸
二盐酸喹吖因
二盐酸喹丫因
英文别名
erion
sn390
mecryl
866r.p.
palusan
ATABRINE
italchin
metochin
metoquin
palacrin

物理化学性质

熔点249-251℃ (Decomposition)
密度1.2962 (rough estimate)
折射率1.6300 (estimate)
储存条件+15C to +30C
酸度系数(pKa)pKa -6.3(H2O t undefined I not reported but low) (Uncertain)
形态黄色固体
PH值3.0~5.0 (20g/l, 25℃)
Merck14,8044
BRN4834013
稳定性稳定的。与强氧化剂不相容。

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302
危险品标志Xn
危险类别码22-36/37/38
安全说明36/37/39
WGK Germany3
RTECS号AR7875000
毒性LD50 oral in rabbit: 433mg/kg
二盐酸奎吖因水合物价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-13735A二盐酸奎吖因水合物
Quinacrine dihydrochloride
69-05-6100mg496元
2024/04/30S4255疟疾平
Quinacrine 2HCl
69-05-650mg800.64元
2024/04/30S4255Quinacrine 2HCl69-05-61g5487.3元

常见问题列表

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。
靶点
TargetValue
PLA2
()
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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