Home>>Signaling Pathways>> DNA Damage/DNA Repair>> Topoisomerase>>Merbarone

Merbarone Sale

(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。

Merbarone Chemical Structure

Cas No.:97534-21-9

规格 价格 库存 购买数量
1mg
¥300.00
现货
5mg
¥1,000.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

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
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
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
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
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
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

产品文档

Quality Control & SDS

View current batch: