Merbarone

Merbarone用途

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。Merbarone 具有抗肿瘤功效。

Merbarone名称

[ CAS 号 ]:
97534-21-9

[ 中文名 ]:
水牛

[ 英文名 ]:
Merbarone

[英文别名 ]:

CC-PMLSC-PW-kmcmerbarone
HMS2198P18

Merbarone生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

[ 靶点 ]

topoisomerase II[1]

[体外研究]

美巴龙(1-100μM)以浓度依赖性方式抑制L1210细胞增殖,IC50为10μM[3]。美巴龙(10-200μM；10分钟)抑制人类拓扑异构酶IIα催化的DNA弛豫,IC50为∼40μM[1]。美巴龙(25-200μM；6分钟)阻断Tyopo异构酶II介导的DNA切割,IC50为∼50μM[1]。美巴龙(100μM；6分钟)以全局方式抑制拓扑异构酶II介导的DNA切割[1]。美巴龙(100μM；6分钟)不损害拓扑异构酶II•DNA结合[1]。美巴龙(200μM；4-16 min)不抑制拓扑异构酶II催化的ATP水解[1]。

[体内研究]

美巴龙(50mg/kg；每日一次,持续5d)可使P388小鼠白血病的最大寿命延长101%。美巴龙(124 mg/kg；每日一次,连续9天)在小鼠体内具有抗肿瘤活性[2]。

[参考文献]

[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.

Merbarone物理化学性质

[ 密度 ]:
1.51g/cm3

[ 分子式 ]:
C₁₁H₉N₃O₃S

[ 分子量 ]:
263.27200

[ 精确质量 ]:
263.03600

[ PSA ]:
119.39000

[ LogP ]:
0.50280

[ 外观性状 ]:
固体

[ 折射率 ]:
1.688

[ 储存条件 ]:
2-8°C，密封，干燥

MerbaroneMSDS

详细MSDS(安全技术说明书)

Merbarone毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV7714625

CHEMICAL NAME :: 5-Pyrimidinecarboxamide, hexahydro-4,6-dioxo-N-phenyl-2-thioxo-

CAS REGISTRY NUMBER :: 97534-21-9

LAST UPDATED :: 199206

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C11-H9-N3-O3-S

MOLECULAR WEIGHT :: 263.29

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 135 mg/kg/5D-I

TOXIC EFFECTS :: Blood - agranulocytosis Blood - thrombocytopenia Blood - changes in bone marrow (not otherwise specified)

REFERENCE :: PAACA3 Proceedings of the American Association for Cancer Research. (Waverly Press, 428 E. Preston St., Baltimore, MD 21202) V.1- 1954- Volume(issue)/page/year: 29,189,1988

Merbarone安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
UV7714625

Merbarone文献

Dominant lethal mutations of topoisomerase II inhibitors etoposide and merbarone in male mice: a mechanistic study.

Arch. Toxicol. 86(5) , 725-31, (2012)

Two topoisomerase II inhibitors, etoposide and merbarone, were tested for the induction of dominant lethal mutations in male mice. Etoposide was administered at a dosage of 30 or 60 mg/kg. Merbarone w...

Merbarone: an antitumor agent entering clinical trials.

Invest. New Drugs 5(2) , 137-43, (1987)

Merbarone was developed to clinical trial stage on the basis of its 'curative' activity against P388 and L1210 leukemias and moderate activity against B16 melanoma and M5076 sarcoma. Its activity appe...

Differential cell cycle-specificity for chromosomal damage induced by merbarone and etoposide in V79 cells.

Mutat. Res. 616(1-2) , 70-82, (2007)

Merbarone, a topoisomerase II (topo II) inhibitor which, in contrast to etoposide, does not stabilize topo II-DNA cleavable complexes, was previously shown to be a potent clastogen in vitro and in viv...

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