Website:www.dcchemicals.com Email: info@dcchemicals.com Phone:+86-21-58447131 Marketing Center: Room 610,Building 15, Jinxiang Rd 201, Shanghai, China
Datasheet of Tirapazamine
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. 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. 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. 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.
Chemical Information Catalog
DC4130
Purity of current batch:
>98%
Molecular Weight (MW)
178.15
Molecular Formula
C7H6N4O2
CAS No.
27314-97-2
Solubility (25°C)
DMSO
Storage
Store at -20°C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.