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Merbarone

CAS No. : 97534-21-9

MCE 站：Merbarone

产品活性：Merbarone (NSC 336628) 是一种具有口服活性的拓扑异构酶 II (topoisomerase II) 抑制剂。Merbarone 的主要作用是阻断拓扑异构酶 II 介导的 DNA 切割，而不会稳定拓扑 II-DNA 共价复合物。Merbarone 具有抗肿瘤功效。

研究领域：Cell Cycle/DNA Damage

作用靶点：Topoisomerase

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

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

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