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Azaserine
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。
Azaserine图片
CAS NO:115-02-6
包装与价格:
包装价格(元)
10mM (in 1mL Water)电议
10mg电议
50mg电议

产品介绍
Azazerine (CI-337) 是谷氨酰胺氨基转移酶的竞争性抑制剂。
Cas No.115-02-6
别名偶氮丝胺酸; CI-337; O-Diazoacetyl-L-serine; P-165
化学名O-(2-diazoacetyl)-L-serine
Canonical SMILESO=C(C=[N+]=[N-])OC[C@H](N)C(O)=O
分子式C5H7N3O4
分子量173.1
溶解度≥ 21.4 mg/mL in Water
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 7 μM: inhibits parasite growth.

Azaserine, as a naturally occurring serine derivative diazo compound, functions as a purine antagonist and structural analogue of glutamine that inhibits enzymatic activities involving in the pathways of glutamine metabolism. Azaserine, an antibiotic and antitumor agent, is used as a potential antineoplastic agent in clinical studies. Azaserine dampens the biosynthesis of purine via reacting with cysteine residues in the enzyme active sites. In addition, azaserine triggers DNA damage by the formation of carboxymethylated bases and O6-methylguanine.

In vitro: Azaserine showed cytotoxicity in Raji cells, which was partly due to inhibition of de novo purine biosynthesis, and the expression of O6-methylguanine-DNA methyltransferase did not provide protection against cell killing, suggesting that O6-methylguanine was not a major contributor to the cytotoxic DNA damage triggered by azaserine. Azaserine killed the Raji hypoxanthine-guanine phosphoribosyltransferas-deficient(HPRT-) Mex- cells. In contrast, the Raji HPRT+ Mex- cells were more resistant to azaserine. Additionally, azaserine blocked the growth of Raji HPRT+ Mex-cells when treated with 300 μM [1].

In vivo: CD-l mice and W/LEW rats were injected intraperitoneally with azaserine at a dose of 10 mg/kg body weight once a week for 5 weeks. After 6 months, compared to the control rats and mice, the azaserine-treated animals had a slightly higher incidence of pancreatic atypical acinar cell nodules (AACN) and the average size of AACN of azaserine-treated animals was larger. In addition, the concentration of [14C] azaserine and/or its metabolites was lower in mouse pancreas than in rat pancreas [2].

References:
[1].  O'Driscoll, M., Macpherson, P., Xu, Y., & Karran, P. The cytotoxicity of DNA carboxymethylation and methylation by the model carboxymethylating agent azaserine in human cells. Carcinogenesis. 1999; 20(9): 1855-1862.
[2].  B. D. Roebuck, Herman S. Lilja, Thomas J. Curphey, Daniel S. Longnecker; Pathologic and Biochemical Effects of Azaserine in Inbred Wistar/Lewis Rats and Noninbred CD-1 Mice. J Natl Cancer Inst. 1980; 65 (2): 383-389.