匹杉琼
中文名称 | 匹杉琼 |
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中文同义词 | 匹克生琼;匹杉琼二马来酸盐;6,9-二[(2-氨乙基)氨基]苯并[G]异喹啉-5,10-二酮;匹杉琼;PIXANTRONEBBR 2778匹杉琼;马来酸匹杉琼;拓扑异构酶Ⅱ抑制剂;化合物 PIXANTRONE |
英文名称 | Pixantrone |
英文同义词 | 6,9-bis((2-aminoethyl)amino)benzo(g)isoquinoline-5,10-dione;pixantrone;6,9-Bis[(2-aminoethyl)amino]benz[g]isoquinoline-5,10-dione;CS-1359;Pixantrone, BBR 2778;BBR-2778;BBR2778;BBR 2778;Benz[g]isoquinoline-5,10-dione, 6,9-bis[(2-aminoethyl)amino]-;Pixantrone diformate salt |
CAS号 | 144510-96-3 |
分子式 | C17H19N5O2 |
分子量 | 325.37 |
EINECS号 | |
相关类别 | 原料药;医药原料药;生物试剂;APIs;Amines;Aromatics;Drug Analogues;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;API |
Mol文件 | 144510-96-3.mol |
结构式 |
匹杉琼 性质
熔点 | >173°C (dec.) |
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沸点 | 650.0±55.0 °C(Predicted) |
密度 | 1.405 |
储存条件 | Refrigerator |
溶解度 | 可溶于DMSO(少许)、甲醇(少许) |
酸度系数(pKa) | 9.34±0.10(Predicted) |
形态 | 固体 |
颜色 | 深蓝色至深蓝色 |
Topoisomerase II
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Pixantrone is a topoisomerase II inhibitor. Pixantrone induces cell death in multiple cancer cell lines independent of cell cycle perturbation, with IC 50 s of 37.3 nM, 126 nM and 136 nM for T47D, MCF-10A and OVCAR5 cells, respectively. Pixantrone induces DNA damage at high concentrations (500 nM) but not at concentrations (100 nM) sufficient to kill PANC1 cells. Pixantrone (25 or 100 nM) induces severe chromosomal aberrations and mitotic catastrophe in PANC1 cells. Pixantrone (100 nM) may disrupt chromosome segregation because of generating merotelic kinetochore attachments that cause chromosome non-disjunction. Pixantrone 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. Pixantrone (0.01-0.2 μM) leads to a concentration-dependent formation of linear DNA through acting on topoisomerase IIα. Pixantrone 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 (27 mg/kg) does not worsen pre-existing moderate degenerative cardiomyopathy in doxorubicin-pretreated mice, by i.v. one dose every 7 days repeated thrice (q7d × 3). Pixantrone (27 mg/kg) causes minimal cardiotoxic in mice following repeated treatment cycles. Moreover, Pixantrone results in less mortality than mitoxantrone in doxorubicin-pretreated mice. Pixantrone (16.25 mg/kg i.v, q7d × 3) modulates Lymph node cells (LNC) responses, and affacts T cell subpopulations in TAChR-immunized Lewis rats. Pixantrone also shows preventive and therapeutic effect in experimental autoimmune myasthenia gravis (EAMG) rats.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-13727A | Pixantrone | 1 mg | 240元 | |
2024/08/19 | HY-13727A | 匹杉琼 Pixantrone dimaleate | 144510-96-3 | 5 mg | 600元 |