Azaserine

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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。

CAS NO:

115-02-6

包装与价格：

包装	价格(元)
25mg	电议
50mg	电议
100mg	电议

产品介绍

化学性质

Storage	Store at -20°C
M.Wt	173.1
Cas No.	115-02-6
Formula	C₅H₇N₃O₄
Synonyms	CI-337,CN 15757,O-Diazoacetyl-L-serine,NSC 742
Solubility	insoluble in DMSO; ≥21.4 mg/mL in H2O
Chemical Name	O-(2-diazoacetyl)-L-serine
Canonical SMILES	O=C(C=[N+]=[N-])OC[C@H](N)C(O)=O
运输条件	蓝冰运输或根据您的需求运输。
一般建议	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。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

试验操作

细胞实验 [1]：
细胞系	Raji 细胞
溶解方法	在DMSO中的溶解度
反应条件	5μM，100μM，200μM，400μM，500μM
应用	Azaserine在Raji细胞中显示出细胞毒性，部分原因是由于从头合成嘌呤生物系统受到抑制，O6-甲基鸟嘌呤-DNA甲基转移酶的表达不能提供抗细胞杀伤的保护作用，这表明O6-甲基鸟嘌呤不是造成细胞毒性的主要因素，是zaserine引发了DNA损伤。
动物实验 [2]：
动物模型	W / LEW近交大鼠和CD-1非近交小鼠
剂量	10 mg/kg（i.p.），一周一次，持续五周
应用	与对照大鼠和小鼠相比，在6个月后，用Azaserine处理的动物的胰腺非典型腺泡细胞结节（AACN）的发生率略高，而用Azaserine处理的动物的AACN的平均大小更大。此外，小鼠胰腺中[14C]氮杂嘌呤和/或其代谢产物的浓度低于大鼠胰腺中的浓度。
注意事项	请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。
References: [1]. O'Driscoll M, Macpherson P, Xu YZ, Karran P. The cytotoxicity of DNA carboxymethylation and methylation by the model carboxymethylating agent azaserine in human cells. Carcinogenesis. 1999 Sep;20(9):1855-62. PubMed PMID: 10469634. [2]. Roebuck BD, Lilja HS, Curphey TJ, Longnecker DS. Pathologic and biochemical effects of azaserine in inbred Wistar/Lewis rats and noninbred CD-1 mice. J Natl Cancer Inst. 1980 Aug;65(2):383-9. PubMed PMID: 6931255.