Quinacrine dihydrochloride (Synonyms:阿的平; Mepacrine dihydrochloride; SN-390 dihydrochloride)
目录号 : KM8499 CAS No. : 69-05-6 纯度 : 98%

Quinacrine (Mepacrine) dihydrochloride 是一种有效的,具有口服活性的抗疟剂 (antimalarial),在体内外均具有抗肿瘤作用。Quinacrine dihydrochloride 抑制 NF-κB 并激活 p53 信号转导,诱导肿瘤细胞发生凋亡 (apoptosis)。

规格 价格 是否有货 数量
100mg
In-stock
500mg
In-stock
1g 询价 In-stock
5g 询价 In-stock

Other Forms of Rapamycin:

KKL Med 的所有产品和服务仅用于科学研究,不能被用于人体,兽医,我们也不向个人提供产品和服务。
生物活性

Quinacrine (Mepacrine) dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the 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 IC50 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.
分子式
C23H32Cl3N3O
分子量
472.88
CAS号
69-05-6
中文名称
奎纳克林二盐酸盐;阿的平;米帕林
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 44 mg/mL (93.05 mM)

H2O : 13.89 mg/mL (29.37 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1147 mL 10.5735 mL 21.1470 mL
5 mM 0.4229 mL 2.1147 mL 4.2294 mL
10 mM 0.2115 mL 1.0574 mL 2.1147 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

临床试验
科研文献
暂无相关参考文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
动物实验计算换算器
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系客服为您提供正确的澄清溶液配方)
+
+
+

计算结果:

工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。