Tirapazamine

Description: Trapazamine (also known as TP, SR-4233; SR259075; Win59075; SR4233) is an experimental adjuvant drug and a DNA-damaging agent that has the potential for the treatment of cervical carcinoma, head and neck cancer. Tirapazamine could downregulate HIF-1alpha expression by decreasing HIF-1alpha protein synthesis when activated to its toxic form preferentially in the hypoxic areas of solid tumors. When combined with chemotherapeutic drugs such as Doxorubicin (DOX) and SN-38 (the active metabolite of irinotecan), trapazamine dramatically inhibited the accumulation of HIF-1alpha protein, decreased the HIF-1alpha transcriptional activation, and impaired the phosphorylation of proteins involved in the homologous recombination repair pathway, ultimately resulting in the synergism of these two drugs.

References: Oxid Med Cell Longev. 2012; 2012:890826; Mol Cancer Ther. 2014 Mar; 13(3):630-42.

SR 4233; SR-4233; SR4233; SR259075; SR-259075; SR 259075; WIN 59075; WIN-59075; WIN59075; NSC130181; NSC-130181; NSC 130181; Tirazone; TP; Tirapazamine;

Chemical Name: 3-aminobenzo[e][1, 2, 4]triazine 1, 4-dioxide

Exact Mass: 178.04908