| Description | Tirapazamine (Win59075) is a potent cytotoxic agent under hypoxic conditions, can induce apoptosis by inducing breaks in single and double-stranded DNA, as well as chromosomal breaks. The compound sensitizes cells to other ionizing radiation and other cytotoxic agents like cisplatin. |
| In vitro | Tirapazamine could downregulate HIF-1α expression by decreasing HIF-1α protein synthesis. The enhanced apoptosis induced by tirapazamine plus SN-38 (the active metabolite of irinotecan) was accompanied by increased mitochondrial depolarization and caspase pathway activation [1]. |
| In vivo | The increased the anticancer efficacy of tirapazamine combined with irinotecan was further validated in a human liver cancer Bel-7402 xenograft mouse model [1]. Rats were intraperitoneally injected six times once a week with tirapazamine in two doses, 5 (5TP) and 10 mg/kg (10TP), while doxorubicin was administered in dose 1.8 mg/kg (DOX). Subsequent two groups received both drugs simultaneously (5TP+DOX and 10TP+DOX). Tirapazamine reduced heart lipid peroxidation and normalized RyR2 protein level altered by doxorubicin [2]. |
| Synonyms | Tirazone, Win59075, SR4233, 替拉扎明, SR259075 |
| molecular weight | 178.15 |
| Molecular formula | C7H6N4O2 |
| CAS | 27314-97-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (280.66 mM) |
| References | 1. Cai T Y, Liu X W, Zhu H, et al. Tirapazamine sensitizes hepatocellular carcinoma cells to topoisomerase I inhibitors via cooperative modulation of hypoxia-inducible factor-1α[J]. Molecular cancer therapeutics, 2013: molcanther. 0490.2013. 2. Sliwinska J, Dudka J, Korga A, et al. Tirapazamine-Doxorubicin Interaction Referring to Heart Oxidative Stress and Ca 2[J]. Oxidative medicine and cellular longevity, 2012, 2012. |
| Citations | 1. Liu C, Jia S, Tu L, et al. GSH-Responsive and Hypoxia-Activated Multifunctional Nanoparticles for Synergetically Enhanced Tumor Therapy. ACS Biomaterials Science & Engineering. 2022 2. Wu Z, Wang Y, Li L, et al.New insights into the antimicrobial action and protective therapeutic effect of tirapazamine towards Escherichia coli-infected mice.International Journal of Antimicrobial Agents.2023: 106923. |