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Pixantrone dimaleate 144675-97-8

简要描述:Pixantrone dimaleate 144675-97-8
Pixantrone is a novel aza-anthracenedione compound with antitumor activity.

  • 产品型号:abs47028026
  • 厂商性质:生产厂家
  • 更新时间:2026-01-13
  • 访  问  量:676

详细介绍

品牌absinCAS144675-97-8
分子式C17H19N5O2.2C4H4O4纯度98%
分子量557.21货号abs47028026
规格5mg供货周期现货
主要用途is a novel aza-anthracenedione应用领域化工,生物产业,农林牧渔,制药/生物制药,综合

Pixantrone dimaleate 144675-97-8

产品描述
描述

Pixantrone is a novel aza-anthracenedione compound with antitumor activity. It is a weak topoisomerase II inhibitor and forms stable DNA adducts through alkylation with specificity for DNA hypermethylated sites.

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
马来到匹杉琼;BBR 2778 dimaleate
外观
powder
可溶性/溶解性
DMSO :100 mg/mL (179.37 mM)
Water :100 mg/mL (179.37 mM)
生物活性
靶点
Topoisomerase II
In vitro(体外研究)
Pixantrone dimaleate is a topoisomerase II inhibitor. Pixantrone induces cell death in multiple cancer cell lines independent of cell cycle perturbation, with IC50s 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 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. 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.
In vivo(体内研究)
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.
研究领域
研究领域
CancerDrug resistance
CancerTumor immunology
Drug DiscoverySmall Molecule DrugLead Compound Discovery
Pixantrone dimaleate 144675-97-8温馨提示:本产品仅作科研实验使用,不支持临床等研究

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