Amonafide
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:作用于HT-29、HeLa和PC3细胞的IC50分别为4.67、2.73和6.38。
Amonafide是一种新型的拓扑异构酶II抑制剂。拓扑异构酶II在DNA转录、复制和染色体分离中起重要作用。尽管拓扑异构酶II的生物学功能对于保证基因组的完整性很重要，干扰拓扑异构酶II并生成酶介导的DNA损伤是癌症化疗的有效策略。
体外：Amonafide嵌入DNA并中断拓扑异构酶的作用。与典型药剂相比，amonafide诱导更高分子量的片段，从而导致细胞凋亡而不引起DNA裂解。 Amonafide的作用是ATP非依赖性的，不太可能诱导与治疗引发白血病有关的染色体易位[1]。
体内：Amonafide能抑制IP L1210白血病，16 mg/kg单剂量治疗1至9天，具有61%到106%的最佳生命延长率（ILS）。针对IP P388鼠白血病和SC植入L1210白血病具有类似疗效。另外，针对两个非白血病IP植入小鼠肿瘤M5076肉瘤和黑色素瘤B16，amonafide表现出活性 [2]。
临床试验：针对sAML患者进行了一项多中心、开放性、联合的二期研究，评估连续静脉注射阿糖胞苷和amonafide的疗效。阿糖胞苷输注1-7天，amonafide 600 mg/m2/天1-5天联合用药 [1]。
参考文献：
[1] Freeman CL,Swords R,Giles FJ. Amonafide: a future in treatment of resistant and secondary acute myeloid leukemia Expert Rev Hematol.2012 Feb;5(1):17-26.
[2] Saez R,Craig JB,Kuhn JG,Weiss GR,Koeller J,Phillips J,Havlin K,Harman G,Hardy J,μMelink TJ, et al. Phase I clinical investigation of amonafide. J Clin Oncol.1989 Sep;7(9):1351-8.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 283.33 |
| Cas No. | 69408-81-7 |
| Formula | C16H17N3O2 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥14.17 mg/mL in DMSO |
| Chemical Name | 5-amino-2-[2-(dimethylamino)ethyl]benzo[de]isoquinoline-1,3-dione |
| SDF | Download SDF |
| Canonical SMILES | CN(C)CCN1C(=O)C2=CC=CC3=CC(=CC(=C32)C1=O)N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
化学结构
