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Bisantrene 是一种高效的抗肿瘤药物,靶向作用于真核生物的II型拓扑异构酶 (II topoisomerases)。

比生群名称

[ CAS 号 ]:
78186-34-2

[ 中文名 ]:
比生群

[ 英文名 ]:
Bisantrene

[中文别名 ]:

必桑那

[英文别名 ]:

MFCD01743164
Zantrene
ADAH
BISANTRENE HCL
Orange Crush

比生群生物活性

[ 描述 ]:

Bisantrene 是一种高效的抗肿瘤药物,靶向作用于真核生物的II型拓扑异构酶 (II topoisomerases)。

[ 相关类别 ]:

研究领域 >> 癌症

天然产物 >> 醌类

[ 靶点 ]

Topoisomerase II

[体内研究]

Bisantrene具有与DNA形成复合物的突出能力。 Bisantrene表现出最有效的结合(甚至忽略静电接触),其次是9-取代的化合物,最后是1-IHA。 Bisantrene同源物保留了与单链结构结合的显着能力。与对于双链DNA发现的Ki值相比,9-IHA显示出2倍的增加,1-IHA保持相同的值,并且aza-9-IHA表现出适度的减少。另一方面,Bisantrene虽然经历Ki降低6倍,但仍表现出106M-1量级的亲和常数。 Bisantrene在寡嘌呤-寡嘧啶束上促进DNA酶I切割;相反,它会略微降低交替的嘌呤-嘧啶序列的切割活性[1]。 Bisantrene是一种治疗转移性乳腺癌的活性新药。 Bisantrene是[3H]尿苷掺入RNA和[3H]胸苷掺入DNA的抑制剂[2]。

[激酶实验]

测量在25℃下在ETN缓冲液（1mM EDTA，10mM Tris，pH7.0，用NaCl中）进行，以获得所需的离子强度。在将标量量的DNA加入到新制备的药物溶液中后，分别在配体吸收或发射区域中通过分光光度法或荧光测定法监测结合。为了避免由于消光系数或荧光量子产率的实验误差导致的大的系统不准确性，结合的药物部分的范围是0.15-0.85。评估数据。使用Perkin-Elmer Lambda 5仪器和MPF66荧光计进行光谱测量，两者均配备Haake F3-C恒温器[1]。

[参考文献]

[1]. Sissi C, et al. DNA-binding preferences of Bisantrene analogues: relevance to the sequence specificity of drug-mediated topoisomerase II poisoning. Mol Pharmacol. 1998 Dec;54(6):1036-45.

[2]. Yap HY, et al. Bisantrene, an active new drug in the treatment of metastatic breast cancer. Cancer Res. 1983 Mar;43(3):1402-4.

[相关活性小分子]

比生群物理化学性质

[ 密度 ]:
1.41g/cm3

[ 沸点 ]:
646.3ºC at 760 mmHg

[ 分子式 ]:
C₂₂H₂₂N₈

[ 分子量 ]:
398.46400

[ 闪点 ]:
344.7ºC

[ 精确质量 ]:
398.19700

[ PSA ]:
97.56000

[ LogP ]:
2.06900

[ 折射率 ]:
1.757

[ 储存条件 ]:
库房通风低温干燥,与食品原料分开存放

[ 水溶解性 ]:
deionized water: soluble8mg/mL

比生群MSDS

详细MSDS(安全技术说明书)

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CHEMICAL IDENTIFICATION

RTECS NUMBER :: CA9645000

CHEMICAL NAME :: 9,10-Anthracenedicarboxaldehyde, bis((4,5-dihydro-1H-imidazol-2-yl)hydrazone)-

CAS REGISTRY NUMBER :: 78186-34-2

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C22-H22-N8

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 245 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 46,2703,1986

比生群安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H400

[ 警示性声明 ]:
P273

[ 危害码 (欧洲) ]:
Xn;N

[ 风险声明 (欧洲) ]:
R22;R50/53

[ 安全声明 (欧洲) ]:
S60;S61

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ 海关编码 ]:
2933290090

比生群制备

9，10-蒽二醛和2-肼基-2-咪唑啉二盐酸盐反应，得二盐酸比生群。

比生群海关

[ 海关编码 ]: 2933290090

[ 中文概述 ]:
2933290090. 其他结构含非稠合咪唑环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

比生群文献

In vitro effects of bisantrene on fresh clonogenic leukemia cells: a preliminary study on 15 cases.

Haematologica 75(6) , 527-31, (1990)

In vitro clonogenic assays may be useful for determining the sensitivity of leukemic cells to chemotherapeutic agents. We evaluated the antileukemic effect of Bisantrene (an anthracene derivative now ...

Phase II trial of Bisantrene for metastatic melanoma: an Illinois cancer council study.

Med. Pediatr. Oncol. 19(2) , 126-8, (1991)

Sixteen patients with metastatic melanoma entered this phase II study of the efficacy of monthly cycles of Bisantrene. Toxicity was characterized by leukopenia, resulting in the hospitalization of one...

Retroviral transfer of the human MDR1 gene confers resistance to bisantrene-specific hematotoxicity.

Clin. Cancer Res. 2(6) , 973-80, (1996)

In this work, we demonstrate a protective effect conferred by the human multidrug resistance gene (MDR1) to populations of the murine hematopoietic system against the toxic effects of bisantrene, a no...

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