Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 1,2,4-benzotriazin-3-amine 1,4-dioxide
Purity: ≥98%
Formula Markup: C7H6N4O2
Formula Weight: 178.2
CAS Number: 27314-97-2
Notes: Tirapazamine is a hypoxia-activated anticancer agent.{46027} It is converted to an oxidizing radical under hypoxic conditions and can induce single- and double-strand breaks in DNA, formation of trapped topoisomerase I- and II-DNA complexes, and other chromosomal aberrations, leading to cytotoxicity.{46027,46028,46029} Tirapazamine induces hypoxia-enhanced cytotoxicity in DT40 cells (IC50s = 1.02 and 4.34 μM in hypoxic and normoxic conditions, respectively).{46029} It also induces cytotoxicity in HT-1080 and A549 cells in a concentration-dependent manner under hypoxic conditions.{46027} In vivo, tirapazamine sensitizes tumors to cisplatin (Item No. 13119) in a mouse RIF-1 fibrosarcoma tumor model.{46030} Tirapazamine (0.08 mmol/kg) also sensitizes tumors to fractionated irradiation in a FaDu hypopharyngeal squamous cell carcinoma mouse xenograft model.{46031}
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