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。
| 生物活性 | Pixantrone (BBR 2778 (free base)), a mitoxantrone analog, is atopoisomeraseIIinhibitor and DNA intercalator, with anti-tumor activity. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Pixantrone (0-10 μM, 72 h) induces cell death in multiple cancer cell lines independent of cell cycle perturbation[1].
Pixantrone (25-500 nM, 24 h) 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) 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[2].
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[2].
Pixantrone (0.01-10 μM) 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. |
|
体内研究
(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[3].
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[4].
|
| Clinical Trial | |
| 分子量 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com