Quinacrine dihydrochloride(Synonyms: 阿的平; Mepacrine dihydrochloride; SN-390 dihydrochloride)

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Quinacrine dihydrochloride (Synonyms: 阿的平; Mepacrine dihydrochloride; SN-390 dihydrochloride) 纯度: 99.01%

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)。

Quinacrine dihydrochloride(Synonyms: 阿的平; Mepacrine dihydrochloride; SN-390 dihydrochloride)

Quinacrine dihydrochloride Chemical Structure

CAS No. : 69-05-6

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥605 In-stock
100 mg ￥550 In-stock
500 mg ￥980 In-stock
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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[1].

体外研究
(In Vitro)

Quinacrine (5-20 μM; 24 hours) inhibits the growth of SGC-7901 cells[1].
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[1].
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 [1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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[1]

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
(In Vivo)

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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female SCID mice with acute myeloid leukemia (AML)-PS model[2]
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.

Clinical Trial

分子量

472.88

Formula

C23H32Cl3N3O
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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (sealed storage, away from moisture)。-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。
参考文献

  • [1]. Xiaoyang Wu, et al. Quinacrine Inhibits Cell Growth and Induces Apoptosis in Human Gastric Cancer Cell Line SGC-7901. Curr Ther Res Clin Exp. 2012 Feb;73(1-2):52-64.

    [2]. Anna Eriksson, et al. Towards repositioning of quinacrine for treatment of acute myeloid leukemia – Promising synergies and in vivo effects. Leuk Res. 2017 Dec;63:41-46.

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