1. Cell Cycle/DNA Damage
  2. Topoisomerase

Tirapazamine (Synonyms: SR259075; SR4233; Win59075)

Cat. No.: HY-13767 Purity: 98.07%
Data Sheet SDS Handling Instructions

Tirapazamine(SR259075; Win59075; SR4233) is an experimental anticancer drug that is activated to a toxic radical only at very low levels of oxygen; a phenomenon known as tumor hypoxia.

For research use only. We do not sell to patients.
Tirapazamine Chemical Structure

Tirapazamine Chemical Structure

CAS No. : 27314-97-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
50 mg USD 72 In-stock
100 mg USD 132 In-stock
200 mg USD 240 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Tirapazamine(SR259075; Win59075; SR4233) is an experimental anticancer drug that is activated to a toxic radical only at very low levels of oxygen; a phenomenon known as tumor hypoxia. IC50 value: Target: 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 [1]. in vivo: The combination treatment dramatically inhibited the accumulation of HIF-1α protein, decreased the HIF-1α transcriptional activation, and impaired the phosphorylation of proteins involved in the homologous recombination repair pathway, ultimately resulting in the synergism of these two drugs. Moreover, the increased 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 normalised RyR2 protein level altered by doxorubicin [2].

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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 5.6132 mL 28.0662 mL 56.1325 mL
5 mM 1.1226 mL 5.6132 mL 11.2265 mL
10 mM 0.5613 mL 2.8066 mL 5.6132 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

178.15

Formula

C₇H₆N₄O₂

CAS No.

27314-97-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 39 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.07%

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Tirapazamine
Cat. No.:
HY-13767
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