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 Amonafide
Amonafide
Amonafide
商品货号:CL-10542
CAS 号:69408-81-7
英文名字: Amonafide
质量标准:>98%
分子式:C16H17N3O2
  • 包装规格:
    规格 库存 发货时间
    10mg [¥1550.00]15 现货,一周内发货
    50mg [¥4770.00]15 现货,一周内发货
    100mg [¥8640.00]15 现货,一周内发货
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    商品信息

    质检证书(coa)

    说明书下载

     Amonafide

    分子式C16H17N3O2   分子量283.33

     

    产品描述

    Amonafide (NSC-308847)通过topoisomerase II介导的反应产生蛋白相关的DNA链断裂,但不会产生topoisomerase I介导的DNA裂解。

    靶点

    Topoisomerase II

             

    IC50

               

    体外研究

    Through a topoisomerase II-mediated reaction, Amonafide treatment produces DNA single-strand breaks (SSB), double-strand breaks (DSB), and DNA-protein cross-links in human myeloid leukemia cells. Amonafide treatment inhibits conlony formation of the leukemic cell lines and the normal human bone marrow GM-CFC in a dose-dependent manner. Amonafide does not produce topoisomerase I-mediated DNA cleavage even at 100 μM. The m-AMSA-resistant line is less than 2-fold resistant to Amonafide.Amonafide interferes with the DNA breakage-reunion activity of mammalian DNA topoisomerase II resulting in DNA cleavage stimulation.Compared with those of other antitumor drugs, Amonafide-stimulated cleavage intensity patterns are markedly different. Amonafide highly prefers a cytosine, and excludes guanines and thymines instead, at position -1, with lower preference for an adenine at position +1.Topoisomerase II-mediated DNA cleavage induced by Amonafide is affected only slightly (less than 3-fold) by 1 mM ATP, suggeting that Amonafide is an ATP-insensitive topoisomerase II inhibitor in contrast to doxorubicin, etoposide, and mitoxantrone.Amonafide significantly inhibits the growth of HT-29, HeLa, and PC3 cells with IC50 of 4.67 μM, 2.73 μM, and 6.38 μM, respectively.Amonafide is unaffected by P-glycoprotein-mediated efflux, unlike those of the classical topoisomerase II inhibitors (daunorubicin, doxorubicin, idarubicin, etoposide, and mitoxantrone).

    体内研究

     

    溶解性

    DMSO 57 mg/mL,水 <1 mg/mL,乙醇 4 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

             
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