Amonafide

Research use only, not for human use.

A novel topoisomerase II (Topo II) inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.

A novel topoisomerase II (Topo II) inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.Chemotherapeutic Agents Phase 3 Discontinued(In Vitro):Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA. 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. 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. Amonafide inhibits the growth of HT-29, HeLa, and PC-3 cell lines, with IC50s of 4.67, 2.73, and 6.38 μM.

Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA. 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. 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. Amonafide inhibits the growth of HT-29, HeLa, and PC-3 cell lines, with IC50s of 4.67, 2.73, and 6.38 μM.

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AS1413

Cell Cycle/DNA Damage

Topoisomerase

TopoII

Cancer

Chemotherapeutic

69408-81-7

283.3251

C16H17N3O2

>98% (HPLC)

10 mM in DMSO

O=C1N(CCN(C)C)C(C2=CC(N)=CC3=CC=CC1=C23)=O

1H-Benz[de]isoquinoline-1,3(2H)-dione, 5-amino-2-[2-(dimethylamino)ethyl]-

(-20℃)

With Ice Pack

≥ 2 years