"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.