喹吖因二盐酸 Quinacrine (dihydrochloride) CAS#:69-05-6

您好！欢迎来到化工e站网登陆注册

产品字典

氯化钾 | 乙二醇 | 碘甲烷 | 溴化亚铜 | 叔丁醇钾 | DMAP

结构式搜索

首页化工产品目录原料药抗寄生虫病药抗疟药喹吖因二盐酸

喹吖因二盐酸

产品纠错

CAS号：69-05-6 | 英文名称：Quinacrine (dihydrochloride)

分子式 C₂₃H₃₂Cl₃N₃O

分子量 473

EINECS号 200-700-8

MDL MFCD00012659

Smiles

InChIKey

乙二醇化学百科

基本信息

中文名称	二盐酸奎吖因水合物
英文名称	QUINACRINE DIHYDROCHLORIDE
CAS号	69-05-6
分子式	C23H32Cl3N3O
分子量	472.88
EINECS号	200-700-8

物化性质

熔点	249-251℃ (Decomposition)
密度	1.2962 (rough estimate)
折射率	1.6300 (estimate)
溶解度	可溶于DMSO（轻微）、甲醇（轻微、超声处理）、水（轻微）
形态	黄色固体
酸度系数(pKa)	pKa -6.3(H2Ot undefinedI not reportedbut low) (Uncertain)
颜色	浅黄色至厚黄色
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	稳定的。与强氧化剂不相容。

安全信息

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

生产及用途

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

Target	Value
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.