tcsc0496 Amonafide

Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.

IC50 & Target: Topoisomerase II^[1]

In Vitro: Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA^[1]. Amonafide produces protein-associated DNA cleavage, single-strand breaks (SSB) and DPC and DNA double-strand cleavage. Amonafide (Nafidimide, 400 nM-2.4 μM) reduces the colony-forming ability of the leukemic cell lines in a dose-dependent manner^[2]. Amonafide (0.05-0.4 μg/mL) reduces several tumor growth. However, Amonafide is active against only 12% of tumors compared with standard agents (5-fluorouracil, mitomycin C, cisplatin, and etoposide), which are active against more than 40% of tumors in the human bone marrow inhibitory range^[3]. Amonafide inhibits the growth of HT-29, HeLa, and PC-3 cell lines, with IC₅₀s of 4.67, 2.73, and 6.38 μM^[4].