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Pixantrone free base

CAS No. : 144510-96-3

MCE 站：Pixantrone free base

产品活性：Pixantrone (BBR 2778 (free base)), 米托蒽醌类似物, 是一种拓扑异构酶 II (topoisomerase II) 的抑制剂和 DNA 嵌入剂，具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage

作用靶点：Topoisomerase

In Vitro: 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 semiqui 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.

In Vivo: 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.

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