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编 号：F165524
分子式：C17H19N5O2
分子量：325.37
分子式：C17H19N5O2
分子量：325.37
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CAS No: 144510-96-3
产品详情
生物活性：
Pixantrone (BBR 2778 (free base)), a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
体内研究：
Pixantrone (i.v., 27 mg/kg, every 7 days, three times) 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.Pixantrone (i.v., 16.25 mg/kg, every week, three times) 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.
体外研究：
Pixantrone (0-10 μM, 72 h) induces cell death in multiple cancer cell lines independent of cell cycle perturbation.Pixantrone (25-500 nM, 24 h) can induce DNA damage, hinder chromosome segregation, and induce severe chromosomal aberrations and mitotic catastrophes in PANC1 cells.Pixantrone (0-100 μM, 72 h) potently inhibits growth of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK and ABCB1-transfected MDCK/MDR cells with IC50s of 0.10 μM, 0.56 μM, 0.058 μM and 4.5 μM, respectively.Pixantrone (0.01-0.2 μM) 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.Pixantrone (0.01-10 μM) shows potent inhibitory activities against rat 97-116 peptide-specific T cell proliferation.
Pixantrone (BBR 2778 (free base)), a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
体内研究：
Pixantrone (i.v., 27 mg/kg, every 7 days, three times) 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.Pixantrone (i.v., 16.25 mg/kg, every week, three times) 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.
体外研究：
Pixantrone (0-10 μM, 72 h) induces cell death in multiple cancer cell lines independent of cell cycle perturbation.Pixantrone (25-500 nM, 24 h) can induce DNA damage, hinder chromosome segregation, and induce severe chromosomal aberrations and mitotic catastrophes in PANC1 cells.Pixantrone (0-100 μM, 72 h) potently inhibits growth of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK and ABCB1-transfected MDCK/MDR cells with IC50s of 0.10 μM, 0.56 μM, 0.058 μM and 4.5 μM, respectively.Pixantrone (0.01-0.2 μM) 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.Pixantrone (0.01-10 μM) shows potent inhibitory activities against rat 97-116 peptide-specific T cell proliferation.
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