Pixantrone dimaleate is atopoisomerase II inhibitor and DNA intercalator, with anti-tumor activity. Pixantrone dimaleate is an experimental antineoplastic drug.
Pixantrone dimaleate induces cell death in various cancer cell lines regardless of cell cycle perturbation, with IC50 values of 37.3 nM, 126 nM, and 136 nM for T47D, MCF-10A, and OVCAR5 cells, respectively, after treatment with concentrations ranging from 0 to 10 μM for 72 hours [1]. Pixantrone dimaleate induces DNA damage at a high concentration of 500 nM after treatment for 24 hours, leading to severe chromosomal aberrations and mitotic catastrophe in PANC1 cells [1]. Pixantrone dimaleate at a concentration of 100 nM for 24 hours may interfere with chromosome segregation by generating merotelic kinetochore attachments, leading to chromosome non-disjunction [1]. Pixantrone dimaleate exhibits potent growth inhibition of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK, and ABCB1-transfected MDCK/MDR cells, with IC50 values of 0.10 μM, 0.56 μM, 0.058 μM, and 4.5 μM, respectively, after treatment with concentrations ranging from 0 to 100 μM for 72 hours [2]. Pixantrone dimaleate (0.01-0.2 μM) induces the concentration-dependent formation of linear DNA by targeting topoisomerase IIα and generates semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, possibly due to low cellular uptake [2]. Pixantrone dimaleate (0.01-10 μM) exhibits strong inhibitory effects on rat 97-116 peptide-specific T cell proliferation [4].
体内研究
Pixantrone dimaleate administered intravenously at a dose of 27 mg/kg, given every 7 days for three cycles, does not exacerbate pre-existing moderate degenerative cardiomyopathy in mice. Furthermore, it induces minimal cardiotoxicity upon repeated treatment cycles and leads to lower mortality rates compared to Mitoxantrone in mice pre-treated with Doxorubicin [3].
Pixantrone dimaleate administered intravenously at a dose of 16.25 mg/kg, given weekly for three cycles, alters the responses of lymph node cells (LNC) and affects T cell subpopulations in TAChR-immunized Lewis rats. Additionally, it demonstrates both preventive and therapeutic effects in experimental autoimmune myasthenia gravis (EAMG) rats [4].
体外研究
Pixantrone dimaleate induces cell death in various cancer cell lines regardless of cell cycle perturbation, with IC50 values of 37.3 nM, 126 nM, and 136 nM for T47D, MCF-10A, and OVCAR5 cells, respectively, after treatment with concentrations ranging from 0 to 10 μM for 72 hours [1].
Pixantrone dimaleate induces DNA damage at a high concentration of 500 nM after treatment for 24 hours, leading to severe chromosomal aberrations and mitotic catastrophe in PANC1 cells [1].
Pixantrone dimaleate at a concentration of 100 nM for 24 hours may interfere with chromosome segregation by generating merotelic kinetochore attachments, leading to chromosome non-disjunction [1].
Pixantrone dimaleate exhibits potent growth inhibition of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK, and ABCB1-transfected MDCK/MDR cells, with IC50 values of 0.10 μM, 0.56 μM, 0.058 μM, and 4.5 μM, respectively, after treatment with concentrations ranging from 0 to 100 μM for 72 hours [2].
Pixantrone dimaleate (0.01-0.2 μM) induces the concentration-dependent formation of linear DNA by targeting topoisomerase IIα and generates semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, possibly due to low cellular uptake [2].
Pixantrone dimaleate (0.01-10 μM) exhibits strong inhibitory effects on rat 97-116 peptide-specific T cell proliferation [4].
United States, Arizona
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Arizona Clinical Research Center
Tucson, Arizona, United States, 85712
United States, Arkansas
Highlands Oncology Group
Springdale, Arkansas, United States, 72764
United States, California
USC/Norris Comprehensive Cancer Center and Hospital
Los Angeles, California, United States, 90033-0800
United States, Maryland
Marlene and Stewart Greenebaum Cancer Center, University of Maryland
Baltimore, Maryland, United States, 21201
United States, Ohio
Ireland Cancer Center
Cleveland, Ohio, United States, 44106-5055
United States, Tennessee
Boston Baskin Cancer Group, University Tennessee
Memphis, Tennessee, United States, 38104
United States, Texas
University of Texas - MD Anderson Cancer Center
Houston, Texas, United States, 77030 收起 <<
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