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Amonafide Sale

(Synonyms: 氨萘非特; AS1413) 目录号 : GC11019

A DNA-intercalating topoisomerase II poison

Amonafide Chemical Structure

Cas No.:69408-81-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥578.00
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5mg
¥525.00
现货
25mg
¥1,386.00
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100mg
¥3,476.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

In experiments measuring survival following 1 h drug treatments, 2 × 106cells are resuspended in 2 mL warm (37°C) HBSS with 5% PCS; the appropriate drug (Amonafide) level is attained with the addition of less than 50 μL. Cells are incubated for 60 min at 37°C after which 10 mL ice cold PBS is added. The cells are then centrifuged at 200 × g for 10 min at 4°C. The wash is repeated once and the cells are resuspended in HBSS with 5% PCS and added to the agar-medium mixture for assessment of surviving clonogenic cells[2].

References:

[1]. Allen SL, et al. Amonafide: a potential role in treating acute myeloid leukemia. Expert Opin Investig Drugs. 2011 Jul;20(7):995-1003.
[2]. Andersson BS, et al. In vitro toxicity and DNA cleaving capacity of benzisoquinolinedione (nafidimide; NSC 308847) in human leukemia. Cancer Res. 1987 Feb 15;47(4):1040-4.
[3]. Ajani JA, et al. In vitro activity of amonafide against primary human tumors compared with the activity of standard agents. Invest New Drugs. 1988 Jun;6(2):79-85.

产品描述

IC50: 4.67, 2.73, and 6.38 for HT-29, HeLa, and PC3 cells, respectively

Amonafide is a novel topoisomerase II inhibitor. Topoisomerase II plays critical roles including DNA transcription, replication and chromosome segregation. Though the biological functions of topoisomerase II are important for insuring genomic integrity, the ability to interfere with topoisomerase II and generate enzyme mediated DNA damage is an effective strategy for cancer chemotherapy.

In vitro: Amonafide intercalated with DNA and disrupted the loading of topoisomerases. In contrast to the classic agents, amonafide was found to induce higher molecular weight fragmentation, resulting in the apoptosis without DNA cleavage. Amonafide was found to act in an ATP-independent manner and seemed unlikely to induce the chromosome translocations associated with treatmentinduced leukemia [1].

In vivo: Amonafide was found to be able to inhibit IP L1210 leukemia, with optimal increased life spans (ILS) of 61% to 106% following single 16 mg/kg dosing on days 1 to 9. Similar efficacy was noted against IP P388 murine leukemia and the SC implanted L1210 leukemia. Additionally, amonafide demonstrated activity against two nonleukemic IP implanted murine tumors, the M5076 sarcoma and the B16 melanoma [2].

Clinical trial: A multicenter, open-label, combination Phase II study was conducted for patients with sAML, evaluating the efficacy of cytarabine and amonafide administered as a continuous iv. Infusion of cytarabine on days 1-7 combined with 600 mg/m2/day for days 1-5[1].

References:
[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,Melink TJ, et al.  Phase I clinical investigation of amonafide. J Clin Oncol.1989 Sep;7(9):1351-8.

Chemical Properties

Cas No. 69408-81-7 SDF
别名 氨萘非特; AS1413
化学名 5-amino-2-[2-(dimethylamino)ethyl]benzo[de]isoquinoline-1,3-dione
Canonical SMILES CN(C)CCN1C(=O)C2=CC=CC3=CC(=CC(=C32)C1=O)N
分子式 C16H17N3O2 分子量 283.33
溶解度 ≥ 14.2mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.5295 mL 17.6473 mL 35.2945 mL
5 mM 0.7059 mL 3.5295 mL 7.0589 mL
10 mM 0.3529 mL 1.7647 mL 3.5295 mL
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