A hypoxia-activated anticancer agent; is converted to an oxidizing radical under hypoxic conditions; can induce single- and double-strand breaks in DNA

Tirapazamine – 250 mg

Brand:
Cayman
CAS:
27314-97-2
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

A hypoxia-activated anticancer agent; is converted to an oxidizing radical under hypoxic conditions; 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; induces hypoxia-enhanced cytotoxicity in DT40 cells (IC50s = 1.02 and 4.34 μM in hypoxic and normoxic conditions, respectively); induces cytotoxicity in HT-1080 and A549 cells in a concentration-dependent manner under hypoxic conditions; sensitizes tumors to cisplatin in a mouse RIF-1 fibrosarcoma tumor model; sensitizes tumors to fractionated irradiation in a FaDu hypopharyngeal squamous cell carcinoma mouse xenograft model at (0.08 mmol/kg)

Formal name: 1,2,4-benzotriazin-3-amine 1,4-dioxide

Synonyms:  3-Amino-1,2,4-benzotriazine 1,4-Dioxide|SR 259075|SR 4233|WIN 59075

Molecular weight: 178.2

CAS: 27314-97-2

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals||Research Area|Cancer|Cell Death||Research Area|Cancer|DNA Damage and Repair||Research Area|Oxidative Stress & Reactive Species|DNA/RNA Oxidative Damage

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