货号:A391656
同义名:
AS1413;Benzisoquinolinedione
Amonafide produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage.
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产品名称 | Topo I ↓ ↑ | Topo II ↓ ↑ | Topo IV ↓ ↑ | Topoisomerase ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ellagic acid | ✔ | 99%+ | |||||||||||||||||
β-Lapachone | ✔ | 99%+ | |||||||||||||||||
(s)-10-hydroxycamptothecin | ✔ | 99%+ | |||||||||||||||||
Camptothecin |
++
Topo I, IC50: 0.68 μM |
98% | |||||||||||||||||
Betulinic acid |
++
Eukaryotic topoisomerase I, IC50: 5 μM |
99%+ | |||||||||||||||||
Topotecan |
++++
Topo I (DU-145 Luc cells), IC50: 2 nM Topo I (MCF-7 Luc cells), IC50: 13 nM |
99%+ | |||||||||||||||||
Irinotecan HCl Trihydrate | ✔ | 98% | |||||||||||||||||
SN-38 | ✔ | 98% | |||||||||||||||||
Levofloxacin hydrate | ✔ | 99%+ | |||||||||||||||||
Dexrazoxane | ✔ | 99%+ | |||||||||||||||||
Ofloxacin | ✔ | 98+% | |||||||||||||||||
Enoxacin | ✔ | 99%+ | |||||||||||||||||
Flumequine |
+
Topo II, IC50: 15 μM |
99%+ | |||||||||||||||||
Levofloxacin | ✔ | 99%+ | |||||||||||||||||
Etoposide | ✔ | 98% | |||||||||||||||||
Pefloxacin mesylate dihydrate | ✔ | 99+% | |||||||||||||||||
Marbofloxacin | ✔ | 99%+ | |||||||||||||||||
Voreloxin HCl | ✔ | 98% | |||||||||||||||||
Mitoxantrone dihydrochloride | ✔ | PKC | 99%+ | ||||||||||||||||
Nalidixic acid | ✔ | 99%+ | |||||||||||||||||
Doxorubicin | ✔ | 98% | |||||||||||||||||
Novobiocin sodium | ✔ | 98%+ | |||||||||||||||||
Amonafide | ✔ | 99%+ | |||||||||||||||||
Pirarubicin | ✔ | 98%+ | |||||||||||||||||
Idarubicin HCl |
+++
Topo II (MCF-7 cells), IC50: 3.3 ng/mL |
99%+ | |||||||||||||||||
Genistein | ✔ | EGFR | 98% | ||||||||||||||||
Teniposide | ✔ | 98% | |||||||||||||||||
Moxifloxacin | ✔ | 98% | |||||||||||||||||
Ciprofloxacin | ✔ | 99%+ | |||||||||||||||||
Clinafloxacin | ✔ | 97% | |||||||||||||||||
Gatifloxacin | ✔ | 99%+ | |||||||||||||||||
Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
Epirubicin HCl | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Topoisomerase II (topo II) is an enzyme essential for chromosome segregation and DNA supercoiling homeostasis[3]. Amonafide is a novel topoisomerase II (Topo II) inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA[4]. In vitro, P-glycoprotein (Pgp)-mediated transport (efflux) of amonafide from myeloblasts obtained from patients with secondary acute myeloid leukemia (sAML) was significantly less than efflux of daunorubicin[4]. Amonafide produces protein-associated DNA cleavage, single-strand breaks (SSB) and DPC and DNA double-strand cleavage. Amonafide (400 nM-2.4 μM) reduces the colony-forming ability of the leukemic cell lines in a dose-dependent manner[5]. Amonafide has shown efficacy in patients with sAML, as well as in patients with poor prognostic characteristics such as older age and unfavorable cytogenetics, all associated with drug resistance (MDR). Improved antileukemic activity is observed when amonafide is given together with cytarabine, rather than as monotherapy, with a complete remission rate of ∼ 40% in a recent Phase II trial in sAML[4]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00273884 | Acute Myeloid Leukemia | Phase 2 | Completed | - | - |
NCT00074100 | Breast Cancer | Phase 2 | Completed | - | United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 收起 << |
NCT00087854 | Prostate Cancer | Phase 1 Phase 2 | Completed | - | United States, California ... 展开 >> USC Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Maryland Cancer Center at John Hopkins Baltimore, Maryland, United States, 21231 United States, Missouri Barnard Cancer Center St.Louis, Missouri, United States, 63110 United States, New Jersey Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08901 United States, New York Herbert Irving Cancer Center New York, New York, United States, 10032-3789 United States, Ohio The Cleveland Clinic Cleveland, Ohio, United States, 44195 United States, Pennsylvania Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111-2497 United States, Washington Seattle Cancer Care Alliance Seattle, Washington, United States, 98109 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.53mL 0.71mL 0.35mL |
17.65mL 3.53mL 1.76mL |
35.30mL 7.06mL 3.53mL |
CAS号 | 69408-81-7 |
分子式 | C16H17N3O2 |
分子量 | 283.325 |
别名 | AS1413;Benzisoquinolinedione;Xanafide;Quinamed;NSC 308847;NCI 308847;Nafidimide |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 40 mg/mL(141.18 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |