Tirapazamine

CAS号

27314-97-2

分子式

C7H6N4O2

主要靶点

Others

仅限科研使用

Cat No : CM05618

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Synonyms

Bioreductive Agent|Anticancer Agent|inhibit|替拉扎明|SR 259075|SR 4233|SR4233|SR-4233|SR259075|SR-259075|SML 0552|SML0552|SML-0552|Tirapazamine|Tirazone|Win 59075|Win59075|Win-59075|Inhibitor



产品信息

CAS号 27314-97-2
分子式 C7H6N4O2
主要靶点 Others
主要通路 其他
分子量 178.15
纯度 99.87%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 keep away from moisture,store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Bioreductive Agent|Anticancer Agent|inhibit|替拉扎明|SR 259075|SR 4233|SR4233|SR-4233|SR259075|SR-259075|SML 0552|SML0552|SML-0552|Tirapazamine|Tirazone|Win 59075|Win59075|Win-59075|Inhibitor

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].

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].

溶解度

DMSO:50 mg/mL (280.66 mM)

参考文献

1.Cai T Y, Liu X W, Zhu H, et al. Tirapazamine sensitizes hepatocellular carcinoma cells to topoisomerase I inhibitors via cooperative modulation of hypoxia-inducible factor-1α[J]. Molecular cancer therapeutics, 2013: molcanther. 0490.2013.
2.Sliwinska J, Dudka J, Korga A, et al. Tirapazamine-Doxorubicin Interaction Referring to Heart Oxidative Stress and Ca< sup> 2[J]. Oxidative medicine and cellular longevity, 2012, 2012.

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