"目录号: HY-13735A
Metabolic Enzyme/ProteaseAutophagy-
Quinacrine是一种荧光探针，使胆碱能受体蛋白发生构象转变，低μM水平对AML细胞具有作用活性，平均IC50为2.30 μM。
PhospholipaseAutophagy
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生物活性
Description
Quinacrine is a fluorescent probe for the conformational transitions of the cholinergic receptor protein. Quinacrine shows activity in the low μM range with a mean IC50 of 2.30 μM In the patient AML cells.IC50 value: 2.30 μM (for AML cells)Target:in vitro: Quinacrine is a fluorescent probe for the conformational transitions of the cholinergic receptor protein in its membrane-bound state.[1] In the patient AML samples, Quinacrine showed activity in the low μM range with a mean IC50 of 2.30 μM, statistically significantly lower than that of normal PBMCs; 3.54 μM (P=0.0327; Student's t-test). Samples from patients with chronic lymphocytic, acute myeloid and lymphocytic leukemias as well as peripheral blood mononuclear cells (PBMC) were tested in response to 1266 compounds from the LOPAC1280 library. 25 compounds were defined as hits with activity in all leukemia subgroups (<50% cell survival compared with control) at 10 μM drug concentration. Only Quinacrine showed concurrent high activity in all leukemia subgroups and low activity in normal PBMCs and was, therefore, selected for further preclinical evaluation. Quinacrine also induced early inhibition of both DNA and protein synthesis. Quinacrine have repositioning potential for treatment of acute myeloid leukemia by targeting of ribosomal biogenesis.[2]
Clinical Trial
NCT00417274
Cleveland BioLabs
Prostatic Cancer
December 2006
Phase 2
NCT01844076
Milton S. Hershey Medical Center
Colorectal Adenocarcinoma
March 2014
Phase 1-Phase 2
NCT00183092
University of California, San Francisco-National Institute on Aging (NIA)
Creutzfeldt-Jakob Disease
April 2005
Phase 2
NCT01839955
Neelesh Sharma MD PhD-Case Comprehensive Cancer Center
Recurrent Non-small Cell Lung Cancer-Stage IIIB Non-small Cell Lung Cancer-Stage IV Non-small Cell Lung Cancer
September 2013
Phase 1
NCT00104663
Medical Research Council
Prion Disease
June 2004
NCT00574483
Cleveland BioLabs
Renal Cell Carcinoma
November 2007
Phase 2
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References
[1].Grünhagen HH, et al. Studies on the electrogenic action of acetylcholine with Torpedo marmorata electric organ. IV. Quinacrine: a fluorescent probe for the conformational transitions of the cholinergic receptor protein in its membrane-bound state. J Mol Biol. 1976 Sep 25;106(3):497-516.
[2].Eriksson A, et al. Drug screen in patient cells suggests quinacrine to be repositioned for treatment of acute myeloid leukemia.Blood Cancer J. 2015 Apr 17;5:e307.