化合物 Pixantrone hydrochloride T61351

Product Introduction
Bioactivity


英文名: Pixantrone hydrochloride

描述: Pixantrone (BBR 2778 (free base)) hydrochloride is a mitoxantrone analog compound that acts as a topoisomerase II inhibitor and DNA intercalator. It displays anti-tumor activity [1] [2].

体外活性: Pixantrone (0-10 μM, 72 h) hydrochloride induces cell death in multiple cancer cell lines independent of cell cycle perturbation [1]. Pixantrone (25-500 nM, 24 h) hydrochloride can induce DNA damage, hinder chromosome segregation, and induce severe chromosomal aberrations and mitotic catastrophes in PANC1 cells [1]. Pixantrone (0-100 μM, 72 h) hydrochloride potently inhibits growth of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK and ABCB1-transfected MDCK/MDR cells with IC 50 s of 0.10 μM, 0.56 μM, 0.058 μM and 4.5 μM, respectively [2]. Pixantrone (0.01-0.2 μM) hydrochloride leads to a concentration-dependent formation of linear DNA through acting on topoisomerase IIα and produces semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, most likely due to low cellular uptake [2]. Pixantrone (0.01-10 μM) hydrochloride shows potent inhibitory activities against rat 97-116 peptide-specific T cell proliferation [4]. Cell Proliferation Assay [1] Cell Line: T47D, MCF-10A and OVCAR5 cells Concentration: 0-10 μM Incubation Time: 72 h Result: Reduced the proliferation of T47D, MCF-10A and OVCAR5 cells with 37.3 nM, 126 nM and 136 nM, respectively. Cell Proliferation Assay [4] Cell Line: Lewis rat T cell lines Concentration: 0.01-10 μM Incubation Time: Result: Inhibited 39.3% rat 97-116 peptide-specific T cells proliferation at 0.01 μM and completely suppressed T cell proliferation at high concentrations.

体内活性: Pixantrone (i.v., 27 mg/kg, every 7 days, three times) hydrochloride does not worsen pre-existing moderate degenerative cardiomyopathy, causes minimal cardiotoxic in mice following repeated treatment cycles and results in less mortality than mitoxantrone in doxorubicin-pretreated mice [3]. Pixantrone (i.v., 16.25 mg/kg, every week, three times) hydrochloride modulates Lymph node cells (LNC) responses, affacts T cell subpopulations in TAChR-immunized Lewis rats and also shows preventive and therapeutic effect in experimental autoimmune myasthenia gravis (EAMG) rats [4].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途