Azaserine
(Synonyms: 偶氮丝胺酸; CI-337; O-Diazoacetyl-L-serine; P-165) 目录号 : GC14874
A glutamine antagonist with anti-tumorigenic activity
Cas No.:115-02-6
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 115-02-6 | SDF | |
| 别名 | 偶氮丝胺酸; CI-337; O-Diazoacetyl-L-serine; P-165 | ||
| 化学名 | O-(2-diazoacetyl)-L-serine | ||
| Canonical SMILES | O=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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.777 mL | 28.885 mL | 57.7701 mL |
| 5 mM | 1.1554 mL | 5.777 mL | 11.554 mL |
| 10 mM | 0.5777 mL | 2.8885 mL | 5.777 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet