中文名 | Tretazicar |
英文名 | Tretazicar |
别名 | 4-二硝基苯甲酰胺 5-(1-氮杂环丙基)-2 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 |
英文别名 | CB-954 CB-1954 CB 1954 tretazicar Tretazicar NSC 115829 5-Aziridino-2,4-dinitrobenzamide 5-(1-aziridinyl)-2,4-dinitrobenzamide 2,4-Dinitro-5-(aziridine-1-yl)benzamide 5-(1-Aziridinyl)-2,4-dinitrobenzamide, 5-(Aziridin-1-yl)-2,4-dinitrobenzamide |
CAS | 21919-05-1 |
化学式 | C9H8N4O5 |
分子量 | 252.18 |
InChIKey | WOCXQMCIOTUMJV-UHFFFAOYSA-N |
密度 | 1.671±0.06 g/cm3(Predicted) |
熔点 | 173 °C |
沸点 | 427.2±45.0 °C(Predicted) |
溶解度 | 乙腈 (微溶),DMSO (微溶),乙酸乙酯 (微溶),甲醇 (Sl |
酸度系数 | 14.23±0.50(Predicted) |
存储条件 | -20°C |
外观 | 固体 |
颜色 | Yellow to Dark Yellow |
体外研究 | NOR1过表达可将单一功能烷化剂CB1954转化为其毒性形式。具有细胞毒性的CB1954增强NPC细胞系CNE1的细胞杀伤。NOR1基因在HepG2细胞中可通过上调Grb2的表达和激活MAPK信号转导来增强CB1954所介导的细胞毒性。 |
体内研究 | NTR/CB1954系统在体内用来进行细胞特异性消融实验。这一诱导性消融系统具有剂量依赖性效果。这一过程不需要细胞增殖,活化的CB1954与DNA交联,引起细胞凋亡级联,致使细胞快速死亡。NTR-CB1954系统诱导的特异性细胞消融不需要通过功能性p53途径。 |
WGK Germany | 3 |
参考资料 展开查看 | 1: Prosser GA, Copp JN, Mowday AM, Guise CP, Syddall SP, Williams EM, Horvat CN, Swe PM, Ashoorzadeh A, Denny WA, Smaill JB, Patterson AV, Ackerley DF. Creation and screening of a multi-family bacterial oxidoreductase library to discover novel nitroreductases that efficiently activate the bioreductive prodrugs CB1954 and PR-104A. Biochem Pharmacol. 2013 Apr 15;85(8):1091-103. doi: 10.1016/j.bcp.2013.01.029. Epub 2013 Feb 8. PubMed PMID: 23399641. 2: Swe PM, Copp JN, Green LK, Guise CP, Mowday AM, Smaill JB, Patterson AV, Ackerley DF. Targeted mutagenesis of the Vibrio fischeri flavin reductase FRase I to improve activation of the anticancer prodrug CB1954. Biochem Pharmacol. 2012 Sep 15;84(6):775-83. doi: 10.1016/j.bcp.2012.07.002. Epub 2012 Jul 14. PubMed PMID: 22796568. 3: Prosser GA, Patterson AV, Ackerley DF. uvrB gene deletion enhances SOS chromotest sensitivity for nitroreductases that preferentially generate the 4-hydroxylamine metabolite of the anti-cancer prodrug CB1954. J Biotechnol. 2010 Oct 1;150(1):190-4. doi: 10.1016/j.jbiotec.2010.08.007. Epub 2010 Aug 19. PubMed PMID: 20727918. 4: Prosser GA, Copp JN, Syddall SP, Williams EM, Smaill JB, Wilson WR, Patterson AV, Ackerley DF. Discovery and evaluation of Escherichia coli nitroreductases that activate the anti-cancer prodrug CB1954. Biochem Pharmacol. 2010 Mar 1;79(5):678-87. doi: 10.1016/j.bcp.2009.10.008. Epub 2009 Oct 21. PubMed PMID: 19852945. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.965 ml | 19.827 ml | 39.654 ml |
5 mM | 0.793 ml | 3.965 ml | 7.931 ml |
10 mM | 0.397 ml | 1.983 ml | 3.965 ml |
5 mM | 0.079 ml | 0.397 ml | 0.793 ml |
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