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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
, orange to dark orange-red
溶解性
DMSO: 10 mg/mL, clear
运输
wet ice
储存温度
−20°C
SMILES字符串
Nc1n[n+]([O-])c2ccccc2[n+]1[O-]
InChI
1S/C7H6N4O2/c8-7-9-11(13)6-4-2-1-3-5(6)10(7)12/h1-4H,(H2,8,9)
InChI key
ORYDPOVDJJZGHQ-UHFFFAOYSA-N
应用
已经使用替拉扎明评估其对U-251 MG(成胶质细胞瘤细胞系)细胞活力的细胞毒性作用。
生化/生理作用
在低氧条件下,替拉扎明是一种有效的细胞毒性剂,通过诱导单链和双链DNA的断裂以及染色体断裂诱导细胞凋亡。 该化合物可使细胞对其他电离辐射和其他细胞毒性药物(如顺铂)敏感。
在缺氧条件下,替拉扎明是有效的细胞毒性药物。
警示用语:
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Expert opinion on investigational drugs, 9(12), 2889-2901 (2000-11-28)
Tirapazamine is the second clinical anticancer drug (after porfiromycin) that functions primarily as a hypoxia-selective cytotoxin. Hypoxic cells in tumours are relatively resistant to radiotherapy and to some forms of chemotherapy and are also biologically aggressive, thus representing an important
Annals of surgery, 259(4), 750-759 (2013-11-21)
To assess the contribution of hypoxia and bone marrow-derived cells to aggressive outgrowth of micrometastases after liver surgery. Liver surgery generates a microenvironment that fosters aggressive tumor recurrence. These areas are characterized by chronic hypoxia and influx of bone marrow-derived
Anti-cancer drug design, 13(6), 541-573 (1998-10-02)
The enzymology of triapazamine (TPZ, SR 4233, WIN 59075, 3-amino-1,2,4-benzotriazene 1,4-dioxide, Tirazone) has been extensively studied in rodents and to a lesser extent in human systems. While it is clear that the initial reductive step in TPZ activation is enzyme-mediated
British journal of cancer, 67(6), 1163-1170 (1993-06-01)
SR 4233 (3-amino-1,2,4-benzotriazine 1,4-dioxide, WIN 59075, tirapazamine) is the lead compound in a new class of bioreductive anticancer drugs, the benzotriazine di-N-oxides. It is currently undergoing Phase I clinical testing. The preferential tumour cell killing of SR 4233 is a
Expert opinion on drug metabolism & toxicology, 8(12), 1589-1597 (2012-10-05)
Cervical cancer is the second-most common malignancy in women worldwide. Cisplatin was introduced as a radiosensitizer in 1999 to improve chances of survival. Tumor cell hypoxia, however, remains a major limiting factor in the treatment of solid tumors with chemotherapy
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