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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
包装与价格:
包装价格(元)
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
SR259075
Tirazone
Win59075
SR4233
替拉扎明
产品介绍
Tirapazamine 是抗癌剂,对实体瘤中的缺氧细胞具有选择性细胞毒性,促使DNA中的单链和双链断裂,碱基损伤和细胞死亡。

产品描述

Tirapazamine is a potent cytotoxic agent under hypoxic conditions, can induce apoptosis by inducing breaks in single and double-stranded DNA, as well as chromosomal breaks. The compound sensitizes cells to other ionizing radiation and other cytotoxic agents like cisplatin.

体外活性

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].

体内活性

The increased the 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 normalized RyR2 protein level altered by doxorubicin [2].

Cas No.

27314-97-2

分子式

C7H6N4O2

分子量

178.151

别名

SR259075;Tirazone;Win59075;SR4233;替拉扎明;Tirapazamine

储存和溶解度

DMSO:200mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years