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.
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].
Withdrawn(reevaluation of comp... 展开 >>ound development) 收起 <<
January 2008
United States, New York
... 展开 >>
Community Care Physicians
Albany, New York, United States, 12208
United States, North Carolina
ClinWorks Cancer Research Center
Charlotte, North Carolina, United States, 28207 收起 <<
Withdrawn(reevaluation of comp... 展开 >>ound development) 收起 <<
January 2008
United States, New York
... 展开 >>
Community Care Physicians
Albany, New York, United States, 12208
United States, North Carolina
ClinWorks Cancer Research Center
Charlotte, North Carolina, United States, 28207 收起 <<
United States, Pennsylvania
... 展开 >>
Fox Chase Cancer Center
Recruiting
Philadelphia, Pennsylvania, United States, 19011
Contact: Wafik El-Deiry 215-214-4233
Principal Investigator: Wafik S. El-Deiry, MD 收起 <<
Recurrent Non-small Cell Lung ... 展开 >>Cancer
Stage IIIB Non-small Cell Lung Cancer
Stage IV Non-small Cell Lung Cancer 收起 <<
Phase 1
Completed
-
United States, Ohio
... 展开 >>
University Hospitals Cleveland Medical Center, Seidman Cancer Center, Case Comprehensive Cancer
Cleveland, Ohio, United States, 44106 收起 <<
搜索
