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97534-21-9

中文名稱 化合物 T28017
英文名稱 MERBARONE
CAS 97534-21-9
分子式 C11H9N3O3S
分子量 263.27
MOL 文件 97534-21-9.mol
更新日期 2025/01/22 09:20:05
97534-21-9 結(jié)構(gòu)式 97534-21-9 結(jié)構(gòu)式

基本信息

中文別名
化合物 T28017
MERBARONE CALBIOCHEM
英文別名
RLBN1001
RLBN-1001
MERBARONE
NSC-336628
Merbarone - CAS 97534-21-9 - Calbiochem
5-(N-PHENYLCARBAMOYL)-2-THIOBARBITURIC ACID
5-(N-PHENYLCARBOXAMIDO)-2-THIOBARBITURIC ACID
5-(N-Phenylcarbamoyl)-2-thiobarbituric acid, NSC-336628
hexahydro-4,6-dioxo-n-phenyl-2-thioxo-5-pyrimidinecarboxamid
4,6-dioxo-N-phenyl-2-sulfanylidene-1,3-diazinane-5-carboxamide

物理化學性質(zhì)

密度1.51±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度二甲基亞砜:>5mg/mL
酸度系數(shù)(pKa)-2.16±0.20(Predicted)
形態(tài)固體
顏色Pink to purple

安全數(shù)據(jù)

WGK Germany3
RTECS號UV7714625

常見問題列表

生物活性
Merbarone (NSC 336628) 是一種具有口服活性的拓撲異構(gòu)酶 II (topoisomerase II) 抑制劑。Merbarone 的主要作用是阻斷拓撲異構(gòu)酶 II 介導的 DNA 切割,而不會穩(wěn)定拓撲 II-DNA 共價復合物。Merbarone 具有抗腫瘤功效。
靶點

topoisomerase II

體外研究

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.

體內(nèi)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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