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97534-21-9

CAS 97534-21-9
分子式 C11H9N3O3S
分子量 263.27
MOL 文件 97534-21-9.mol
更新日期 2024/06/01 22:35:01
97534-21-9 结构式 97534-21-9 结构式

物理化学性质

密度1.51±0.1 g/cm3(Predicted)
储存条件2-8°C
溶解度二甲基亚砜:>5mg/mL
酸度系数(pKa)-2.16±0.20(Predicted)
形态固体

安全数据

WGK Germany3
RTECS号UV7714625

常见问题列表

生物活性
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。
靶点

topoisomerase II

体外研究

Merbarone (1-100 μM) inhibits L1210 cells proliferation in a concentration-dependent manner, with an IC 50 of 10 μM.
Merbarone (10-200 μM; 10 min) inhibits DNA relaxation catalyzed by human topoisomerase IIα, with an IC 50 of ∼40 μM.
Merbarone (25-200 μM; 6 min) blocks tyopoisomerase II-mediated DNA cleavage, with an IC 50 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.

体内研究

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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