|5-(氮丙啶-1-基)-2,4-二硝基苯甲酰胺|CsnPharm

CAS No.: 21919-05-1

5-(Aziridin-1-yl)-2,4-dinitrobenzamide Catalog No. CSN21213

Synonyms: NSC 115829;CB 1954

CB 1954 is an anticancer prodrug used in gene therapy research and is activated by NAD(P)H Quinone Oxidoreductase 2.

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技术信息

生物活性

描述CB 1954 [5-(aziridin-1-yl)-2,4-dinitrobenzamide] is an antitumor prodrug that is activated in certain rat tumors via its 4-hydroxylamine derivative to a potent bifunctional alkylating agent. It is enzymatically activated to generate a difunctional agent, which can form DNA-DNA interstrand crosslinks^[2]. The bioactivation of CB 1954 in rat cells involves the aerobic reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NQO1 (DT-diaphorase)^[3].CD-1 nu/nu mice were initially dosed at 200 mol/kg and showed no signs of toxicity, and a higher dose was assessed and the maximum tolerated doses (MTD) was established at 562mol/kg. None of the mice showed overt toxicity at this dose, although weight loss was observed in some animals^[4].The formation of CB 1954 metabolites was investigated in the liver, plasma and urine of mice and rats dosed at the respective MTD for 4 h post-dose. In mice dosed at the MTD of 562mol/kg, plasma levels of ALT and AST were raised to 6 and 13 times normal levels, respectively, between 3 and 6 days postdose^[5].CB1954 at concentrations of 12.5 and 25 µmol/l increased the sensitization enhancement ratio of HeLa cells to 1.54 and 1.66, respectively. When compared with monotherapy, the combined therapy of NTR/CB1954 and γ‑rays may increase the apoptotic rate and enhance the radiosensitivity of HeLa cells. The combined therapy of γ‑ray radiation and the NTR/CB1954 suicide gene system may be a novel and potent therapeutic method for the treatment of cervical carcinoma^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00746590	Hepatocellular Carcinoma	Phase 2	Terminated(Study terminated pr... more >>ematurely by sponsor for business reason. One patient was enrolled.) Collapse <<	-	Belgium ... more >> Cliniques Universitaires Saint-Luc Brussels, Belgium, 1200 Collapse <<
NCT00746590	-	-	Terminated(Study terminated pr... more >>ematurely by sponsor for business reason. One patient was enrolled.) Collapse <<	-	-

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9654 mL
- 19.8268 mL
- 39.6536 mL
- 5 mM
- 0.7931 mL
- 3.9654 mL
- 7.9307 mL
- 10 mM
- 0.3965 mL
- 1.9827 mL
- 3.9654 mL

技术信息

CAS号

21919-05-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H8N4O5

运输

蓝冰

分子量

252.18

别名

NSC 115829;CB 1954

溶解度

DMSO	50.0 mg/mL (198.3 mM)
Water	insoluble

动物实验配方

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5-(Aziridin-1-yl)-2,4-dinitrobenzamide Catalog No. CSN21213

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