Tirapazamine 是抗癌剂，对实体瘤中的缺氧细胞具有选择性细胞毒性，促使DNA中的单链和双链断裂，碱基损伤和细胞死亡。

Tirapazamine 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.

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].

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].

27314-97-2

C7H6N4O2

178.151

SR259075;Tirazone;Win59075;SR4233;替拉扎明;Tirapazamine

DMSO:200mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years