Tretazicar|21919-05-1|(CB 1954)-陌孚医药/Medlife

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Tretazicar (Synonyms: CB 1954)

目录号: PL03471 纯度: ≥99%

CAS No. :21919-05-1

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中文名称	Tretazicar
中文别名	5-(1-氮杂环丙基)-2,4-二硝基苯甲酰胺;5-(氮丙啶-1-基)-2,4-二硝基苯甲酰胺
英文名称	Tretazicar
英文别名	5-Aziridino-2,4-dinitrobenzamide;5-(1-Aziridinyl)-2,4-dinitrobenzamide;CB-1954;5-(aziridin-1-yl)-2,4-dinitrobenzamide;Tretazicar;1 (5 carbamoyl 2,4 dinitrophenyl)aziridine;2,4-Dinitro-5-ethyleneiminobenzamide;2,4-Dinitroethyleneiminobenzamide;5-(aziridyn-1-yl)-2,4-dinitrobenzamide;5-Aziridinyl-2,4-dinitrobenzamide;CB 1954;CB1954;Tretazicar [INN];Benzamide,5-(1-aziridinyl)-2,4-dinitro-;7865D5D01M;Benzamide, 5-(1-aziridinyl)-2,4-dinitro-;CB1;C9H8N4O5;SMR000326847;5-[aziridin-1-yl]-2,4-dinitrobenzamide;azir;5-(Aziridin-1-yl)-2,4-dinitrobenzamide
Cas No.	21919-05-1
分子式	C₉H₈N₄O₅
分子量	252.18
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months

产品详情	Tretazicar (CB 1954) 是一种抗肿瘤前药，对 Walker 256 大鼠肿瘤细胞系具有很高的效力和选择性。Tretazicar 酶促活化后生成双功能试剂，该试剂可以形成 DNA-DNA 链间交联。大鼠细胞中的 Tretazicar 涉及通过酶 NAD(P)H：醌氧化还原酶1 (NQO1) 将其 4-硝基还原为 4-羟基胺。
生物活性	Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1).
性状	Solid
体外研究(In Vitro)	Tretazicar (CB 1954) (0.1-1000 μM; 3 days) has sensitivity for retrovirally transduced AB22 (AB22-nr) cells with an IC50 of 3 μM. DNA cross-link formation in affected cells is a result of the bioactivation of the drug by the enzyme DT diaphorase (NAD(P)H dehydro-genase (quinone)) in the Walker cells which reduces the 4-nitro group of Tretazicar. The product of this reaction is a difunctional alkylating agent, 5-aziridin-1-yl-4-hydroxylamino-2-nitrobenzamide. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Tretazicar (CB 1954) (80 mg/kg; i.p. on days 2 and 9) results in a significant increase in survival. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c mice (AB22-nr, SKOV3
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；In solvent -80°C 6 months
参考文献	[1]. Knox RJ,et al. Bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) by human NAD(P)H quinone oxidoreductase 2: a novel co-substrate-mediated antitumor prodrug therapy. Cancer Res. 2000 Aug 1;60(15):4179-86. [2]. Knox RJ, et al. CB 1954: from the Walker tumor to NQO2 and VDEPT. Curr Pharm Des. 2003;9(26):2091-104.

溶解度数据	In Vitro: DMSO : 125 mg/mL (495.68 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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