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网站主页 化工产品目录 生物化工 抑制剂 DNA损伤(DNA Damage) Topoisomerase 抑制剂 氨萘非特
  • Amonafide

Amonafide

Amonafide
69408-81-7
￥977.75 1EA 起订
其他 更新日期：2020-01-12

Selleck中国

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联系人：Selleck中国
电话：021-68591985拨打
邮箱：info@selleck.cn

产品详情:

英文名称：
Amonafide
CAS号：
69408-81-7
规格：
10mg/10mM/1mL/50mg/100mg
货号：
S1367
Selleck Chemicals美国品牌，中国库存现货，Topoisomerase抑制剂，CAS#69408-81-7。
更多详情请访问中国唯一官方网站： http://www.selleck.cn/products/Amonafide.html

 

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。
Amonafide;化学试剂

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