二盐酸奎吖因水合物

生物活性靶点体外研究体内研究二盐酸奎吖因水合物试剂级价格

二盐酸奎吖因水合物

CAS号:69-05-6
英文名:QUINACRINE DIHYDROCHLORIDE
中文名:二盐酸奎吖因水合物
CBNumber:CB8320579
分子式:C23H32Cl3N3O
分子量:472.88
MOL File:69-05-6.mol

二盐酸奎吖因水合物化学性质

熔点 :249-251℃ (Decomposition)
密度 :1.2962 (rough estimate)
折射率 :1.6300 (estimate)
储存条件 :+15C to +30C
溶解度 :DMSO (Slightly), Methanol (Slightly, Sonicated), Water (Slightly)
形态 :Yellow solid
酸度系数(pKa) :pKa -6.3(H2O t undefined I not reported but low) (Uncertain)
颜色 :Light Yellow to Yellow
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 :Stable. Incompatible with strong oxidizing agents.
EPA化学物质信息 :Quinacrine hydrochloride (69-05-6)

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

二盐酸奎吖因水合物性质、用途与生产工艺

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.