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Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent[1][2][4].

Merbarone (1-100 μM) inhibits L1210 cells proliferation in a concentration-dependent manner, with an IC50 of 10 μM[3].Merbarone (10-200 μM; 10 min) inhibits DNA relaxation catalyzed by human topoisomerase IIα, with an IC50 of ～40 μM[1].Merbarone (25-200 μM; 6 min) blocks tyopoisomerase II-mediated DNA cleavage, with an IC50 of ～50 μM[1].Merbarone (100 μM; 6 min) inhibits topoisomerase II-mediated DNA cleavage in a global manner[1].Merbarone (100 μM; 6 min) does not impair topoisomerase II?DNA binding[1].Merbarone (200 μM; 4-16 min) does not inhibit topoisomerase II-catalyzed ATP hydrolysis[1].

Merbarone (50 mg/kg; daily i.p. for 5 d) achieves a maximum increased life span (ILS) of 101% in P388 murine leukemia[2].Merbarone (124 mg/kg; daily p.o. for 9 d) has anti-tumor activity in mice[2].

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