氨萘非特 T6336

Product Introduction
Bioactivity


英文名: Amonafide

描述: Amonafide (NSC-308847,AS1413) 是一种拓扑异构酶 II 的抑制剂和 DNA 的嵌入剂，通过拓扑异构酶 II 介导的反应产生蛋白质相关的 DNA 链断裂

细胞实验: 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.(Only for Reference)

体外活性: 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 53 mg/mL (187.1 mM)
Ethanol : 4 mg/mL (14.11 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: NSC308847,AS-1413 | AS 1413 | inhibit | AS-1413 | NSC308847,AS 1413 | Topoisomerase | Inhibitor | Amonafide

相关产品: Mitoxantrone | Topotecan | Enoxacin hydrate | DiPT-4 | Gatifloxacin hydrochloride | Ofloxacin | Tubulin inhibitor 35 | Ellagic acid | SDOX | Sophoridine

相关库: Drug Repurposing Compound Library | Anti-Prostate Cancer Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Clinical Compound Library | Human Metabolite Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library

氨萘非特 T6336信息由TargetMol中国为您提供，如您想了解更多关于氨萘非特 T6336报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途