Merbarone
(Synonyms: NSC 336628) 目录号 : GC61844
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。
Cas No.:97534-21-9
Sample solution is provided at 25 µL, 10mM.
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].
References:
[1]. Fortune JM, et, al. Merbarone inhibits the catalytic activity of human topoisomerase IIalpha by blocking DNA cleavage. J Biol Chem. 1998 Jul 10;273(28):17643-50.
[2]. Brewer AD, et, al. 5-(N-phenylcarboxamido)-2-thiobarbituric acid (NSC 336628), a novel potential antitumor agent. Biochem Pharmacol. 1985 Jun 1;34(11):2047-50.
[3]. Cooney DA, et, al. Initial mechanistic studies with merbarone (NSC 336628). Biochem Pharmacol. 1985 Sep 15;34(18):3395-8.
[4]. Chen M, et, al. Differences in inhibition of chromosome separation and G2 arrest by DNA topoisomerase II inhibitors merbarone and VM-26. Cancer Res. 1995 Apr 1;55(7):1509-16.
Cas No. | 97534-21-9 | SDF | |
别名 | NSC 336628 | ||
Canonical SMILES | O=C(C(C(N1)=O)C(NC1=S)=O)NC2=CC=CC=C2 | ||
分子式 | C11H9N3O3S | 分子量 | 263.27 |
溶解度 | 储存条件 | Store at -20°C | |
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1 mg | 5 mg | 10 mg |
1 mM | 3.7984 mL | 18.9919 mL | 37.9838 mL |
5 mM | 0.7597 mL | 3.7984 mL | 7.5968 mL |
10 mM | 0.3798 mL | 1.8992 mL | 3.7984 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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