Tirapazamine

SKU: orb1302863

Description

Tirapazamine (Win59075) is a hypoxia-activated cytotoxic prodrug that induces DNA single- and double-strand breaks, leading to apoptosis. It functions as a radiosensitizer and chemosensitizer, notably with cisplatin, and is applied in oncology research for studying hypoxia-targeted therapies in vitro and in vivo.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 27314-97-2
• MW: 178.15
• Purity: 99.05% (May vary between batches)
• Formula: C₇H₆N₄O₂
• SMILES: On1c2ccccc2[n+]([O-])nc1=N
• Target: Others
• Solubility: DMSO:51 mg/mL (286.28 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (11.23 mM)

Bioactivity

• 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 . 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 .
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Anticancer Agent, Bioreductive Agent, inhibit, Inhibitor, SML 0552, SML0552, SML-0552, SR 4233, SR 259075, SR4233, SR-4233, SR259075, SR-259075, Tirapazamine, Tirazone, Win 59075, Win59075, Win-59075

Compound Identifiers

PubChem CID

135413511