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Amonafide

In stock
Catalog No.
A2782
DNA intercalator,Topo II inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$79.00
In stock
5mg
$70.00
In stock
25mg
$200.00
In stock
100mg
$470.00
In stock

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Email: [email protected]

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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

Physical AppearanceA solid
StorageStore at -20°C
M.Wt283.33
Cas No.69408-81-7
FormulaC16H17N3O2
Solubility≥14.2mg/mL in DMSO
Chemical Name5-amino-2-[2-(dimethylamino)ethyl]benzo[de]isoquinoline-1,3-dione
SDFDownload SDF
Canonical SMILESCN(C)CCN1C(=O)C2=CC=CC3=CC(=CC(=C32)C1=O)N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

Amonafide