Tirapazamine

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Chemical Structure| 27314-97-2 同义名 : Tirazone; Win59075; 3-Amino-1,2,4-benzotriazine 1,4-Dioxide; SML 0552; SR4233; SR259075
CAS号 : 27314-97-2
货号 : A680596
分子式 : C7H6N4O2
纯度 : 99%+
分子量 : 178.15
MDL号 : MFCD00132954
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Tirapazamine is a novel bioreductive agent with selective cytotoxicity to hypoxic tumour cells, irrespective of their p53 status or apoptotic response, and acts synergistically with cisplatin[3]. Limiting toxicity for tirapazamine at an intravenous dose of 390 mg/m2 was acute, reversible hearing loss. The combination of tirapazamine and cisplatin appears to be safe and effective in the treatment of NSCLC(non-small-cell lung cancer)[4]. The enhanced apoptosis induced by tirapazamine plus SN-38 (the active metabolite of irinotecan) was accompanied by increased mitochondrial depolarization and caspase pathway activation[5]. Tirapazamine reduced heart lipid peroxidation and normalised RyR2 protein level altered by doxorubicin[6]. The correlation between the hypoxic cytotoxic potency of tirapazamine and DNA damage was highly significant[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.61mL

1.12mL

0.56mL

28.07mL

5.61mL

2.81mL

56.13mL

11.23mL

5.61mL
参考文献

[1]Cai TY, Liu XW, et al. Tirapazamine sensitizes hepatocellular carcinoma cells to topoisomerase I inhibitors via cooperative modulation of hypoxia-inducible factor-1α. Mol Cancer Ther. 2014 Mar;13(3):630-42.

[2]Sliwinska J, Dudka J, et al. Tirapazamine-doxorubicin interaction referring to heart oxidative stress and Ca²⁺ balance protein levels. Oxid Med Cell Longev. 2012;2012:890826.

[3]Brown JM. Exploiting tumour hypoxia and overcoming mutant p53 with tirapazamine. Br J Cancer. 1998 Jun;77 Suppl 4(Suppl 4):12-4

[4]Gatzemeier U, Rodriguez G, Treat J, Miller V, von Roemeling R, Viallet J, Rey A. Tirapazamine-cisplatin: the synergy. Br J Cancer. 1998 Jun;77 Suppl 4(Suppl 4):15-7

[5]Cai TY, Liu XW, Zhu H, Cao J, Zhang J, Ding L, Lou JS, He QJ, Yang B. Tirapazamine sensitizes hepatocellular carcinoma cells to topoisomerase I inhibitors via cooperative modulation of hypoxia-inducible factor-1α. Mol Cancer Ther. 2014 Mar;13(3):630-42

[6]Sliwinska J, Dudka J, Korga A, Burdan F, Matysiak W, Jodlowska-Jedrych B, Mandziuk S, Dawidek-Pietryka K. Tirapazamine-doxorubicin interaction referring to heart oxidative stress and Ca²⁺ balance protein levels. Oxid Med Cell Longev. 2012;2012:890826

[7]Siim BG, van Zijl PL, Brown JM. Tirapazamine-induced DNA damage measured using the comet assay correlates with cytotoxicity towards hypoxic tumour cells in vitro. Br J Cancer. 1996 Apr;73(8):952-60