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Tirapazamine (Synonyms: SR259075; SR4233; Win59075)

Cat. No.: HY-13767 Purity: 98.37%
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
Estimated Time of Arrival: December 31
50 mg USD 72 In-stock
Estimated Time of Arrival: December 31
100 mg USD 132 In-stock
Estimated Time of Arrival: December 31
200 mg USD 240 In-stock
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  • Technical Information

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  • 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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Solvent & Solubility
In Vitro: 

DMSO : ≥ 39 mg/mL (218.92 mM)

*"≥" means soluble, but saturation unknown.

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Stock Solutions
Concentration Solvent 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

SMILES

NC1=[N+]([O-])C2=CC=CC=C2[N+]([O-])=N1

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

Purity: 98.37%

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Product Name:
Tirapazamine
Cat. No.:
HY-13767
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Tirapazamine

Cat. No.: HY-13767