您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Tirapazamine
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Tirapazamine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tirapazamine图片
CAS NO:27314-97-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 178.05
Formula C7H6N4O2
CAS No. 27314-97-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 40 mg/mL
Water: <1 mg/mL
Ethanol:
SMILES CodeNC1=[N+]([O-])C2=CC=CC=C2[N+]([O-])=N1
Synonyms

SR 4233; SR-4233; SR4233; SR259075; SR-259075; SR 259075; WIN 59075; WIN-59075; WIN59075; NSC130181; NSC-130181; NSC 130181;Tirazone; TP; Tirapazamine;

Chemical Name: 3-aminobenzo[e][1,2,4]triazine 1,4-dioxide

Exact Mass: 178.04908

实验参考方法
In Vitro

In vitro activity: Trapazamine (also known as SR-4233; SR259075; Win59075; SR4233) is an experimental adjuvant drug and a DNA-damaging agent that has the potential for the treatment of cervical carcinoma, head and neck cancer. Tirapazamine could downregulate HIF-1α expression by decreasing HIF-1α protein synthesis when activated to its toxic form preferentially in the hypoxic areas of solid tumors. When combined with chemotherapeutic drugs such as Doxorubicin (DOX) and SN-38 (the active metabolite of irinotecan), trapazamine 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.


Kinase Assay:


Cell Assay: in combination with tirapazamine, topoisomerase I inhibitors exhibited synergistic cytotoxicity and induced significant apoptosis in several hepatocellular carcinoma cell lines. The enhanced apoptosis induced by tirapazamine plus SN-38 (the active metabolite of irinotecan) was accompanied by increased mitochondrial depolarization and caspase pathway activation. 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.

In VivoThe increased anticancer efficacy of tirapazamine combined with irinotecan was further validated in a human liver cancer Bel-7402 xenograft mouse model.
Animal modelRats
Formulation & DosageRats 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.
References Mol Cancer Ther. 2014 Mar;13(3):630-42; Oxid Med Cell Longev. 2012;2012:890826.