Description: Amonafide dihydrochloride (NSC308847, AS1413) is an imide analogue of naphthalic acid and a potent topoisomerase II (Topo II) inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA. Amonafide produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. 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 .
References: Cancer Res. 1987 Feb 15;47(4):1040-4; Expert Rev Hematol. 2012 Feb;5(1):17-26.
Related CAS #: 69408-81-7 (free base) 150091-68-2 (2HCl) 618863-54-0 (malate) 618863-60-8