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CAS No.: 69-05-6

阿的平 Catalog No. CSN11815

Synonyms: 阿的平;Mepacrine dihydrochloride;SN-390 dihydrochloride

Mepacrine 2HCl is an acridine-derived yellow dye, previously used in the therapy and prevention of malaria and later as an antiprotozoal and immunomodulatory agent. It's also an inhibitor of phospholipase A2.

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技术信息

生物活性

描述Quinacrine dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. 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^[3]. The in vivo use of quinacrine (100mg/kg three times per week for two consecutive weeks) significantly suppressed circulating blast cells at days 30/31 and increased the median survival time (MST). The in vitro drug combination analysis yielded promising synergistic interactions when combining quinacrine with cytarabine, azacitidine and geldanamycin^[4]. Quinacrine 25 mg/kg was shown to protect 70% of mice (statistically significant) from a lethal challenge with mouse-adapted EBOV (Ebola virus) with once-daily intraperitoneal dosing for 8 days^[5]. QA (Quinacrine) demonstrates high degree of cytotoxicity against both immortalized and primary patient-derived cell lines with sub-micromolar 50% inhibitory concentration (IC50) values ranging from 1.2 µM (H2452) to 5.03 µM (H28). Further, QA also inhibited cellular migration and colony formation in MPM cells, demonstrated using scratch and clonogenic assays, respectively^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00574483	Renal Cell Carcinoma	Phase 2	Withdrawn(reevaluation of comp... more >>ound development) Collapse <<	January 2008	United States, New York ... more >> Community Care Physicians Albany, New York, United States, 12208 United States, North Carolina ClinWorks Cancer Research Center Charlotte, North Carolina, United States, 28207 Collapse <<
NCT00183092	-	-	Completed	-	-
NCT00183092	Creutzfeldt-Jakob Disease	Phase 2	Completed	-	United States, California ... more >> University of California, San Francisco San Francisco, California, United States, 94143 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号

69-05-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H32Cl3N3O

运输

蓝冰

分子量

472.88

别名

阿的平;Mepacrine dihydrochloride;SN-390 dihydrochloride

溶解度

DMSO	insoluble
Water	150.0 mg/mL (317.2 mM) warming

动物实验配方

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