Amonafide

Amonafide
  • Amonafide
  • 价格 ¥977.75
  • 包装1EA
  • CAS号69408-81-7
  • 中文名称Amonafide
  • 英文名称Amonafide
  • 发布时间2020/1/12 16:15:37

产品属性

  • 产品英文名称: Amonafide
  • 包装价格: 1EA/977.75RMB
  • 规格: 10mg/10mM/1mL/50mg/100mg
  • 货号: S1367
2020/1/12 16:15:37 Amonafide Amonafide 1EA/977.75RMB 977.75

产品描述

Selleck Chemicals美国品牌,中国库存现货,Topoisomerase抑制剂,CAS#69408-81-7。
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生物活性

产品描述 Amonafide (NSC-308847)通过topoisomerase II(拓扑异构酶II)介导导致蛋白相关的DNA链断裂,但不会产生拓扑异构酶I介导的DNA裂解。Phase 3。
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 

[1]

 Amonafide interferes with the DNA breakage-reunion activity of mammalian DNA topoisomerase II resulting in DNA cleavage stimulation. 

[2]

 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. 

[3]

 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. 

[4]

 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. 

[5]

 Amonafide is unaffected by P-glycoprotein-mediated efflux, unlike those of the classical topoisomerase II inhibitors (daunorubicin, doxorubicin, idarubicin, etoposide, and mitoxantrone). 

[6]

体内研究  
临床实验 A Phase I/II study of Amonafide in men with androgen-independent prostate cancer has been completed.
特征  

细胞试验: 

[5]

细胞系 HT-29, HeLa, and PC3
浓度 Dissolved in DMSO, final concentrations ~10 μM
处理时间 72 hours
方法 All cell lines are in the logarithmic phase of growth when the assay of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) is carried out. Cells are harvested and seeded into 96-well tissue culture plates at a density of 2.5 × 103 cells/well in 150 μL aliquots of medium. The concentrations tested are serial dilutions of a stock solution (10 μM in DMSO) with phosphate-buffered saline (PBS) and are added 24 hours later. The assay is ended after 72 hours of Amonafide exposure and PBS is used as a negative control. After 72 hours treatment, cells are washed twice with PBS, and then 50 μL/well of MTT reagent (1 mg/mL in PBS) together with 150 μL/well of prewarmed medium are added. The plates are returned to the incubator for 4 hours. Subsequently, DMSO is added as solvent. Absorbance is determined at 570 nm with a Microplate reader. All experiments are performed at least three times, and the average of the percentage absorbance is plotted against concentration. Then, the concentration of Amonafide required to inhibit 50% of cell growth (IC50) is calculated for Amonafide.
温馨提示:不可用于临床治疗。
关键字: Amonafide;化学试剂

公司简介

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