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6-diazo-5-oxo-L-nor-Leucine

(Synonyms: 6-重氮-5-氧代-L-正亮氨酸; L-6-Diazo-5-oxonorleucine; DON)

目录号: PC17419 纯度: ≥98%

L-6-Diazo-5-oxonorleucine (L-6-Diazo-5-oxonorleucine) 是一种谷氨酰胺拮抗剂，其Ki 值为 6 μM。L-6-Diazo-5-oxonorleucine 具有镇痛、抗菌、抗病毒和抗癌作用。L-6-Diazo-5-oxonorleucine 在体外表现出遗传毒性。L-6-Diazo-5-oxonorleucine 能降低肿瘤细胞的自我更新能力和转移能力。

CAS No. :157-03-9

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中文名称	6-diazo-5-oxo-L-nor-Leucine
中文别名	6-重氮-5-氧代-L-正白氨酸;6-重氮-5-氧代-L-正亮氨酸;硫鸟嘌呤
英文名称	6-diazo-5-oxo-L-nor-Leucine
英文别名	L-Norleucine,6-diazo-5-oxo-;6-DIAZO-5-OXO-L -NORLEUCINE;H-6-Diazo-5-oxo-Nle-OH;(S)-2-Amino-6-diazo-5-oxocaproic acid,DON;(S)-2-Amino-6-diazo-5-oxocaproic acid;DON;L-DON;D2141;NSC-7365;H-L-Don-OH;don(pharmaceutical);diazo-oxo-norleucine;H-NLE(6-DIAZO-5-OXO)-OH;L-Nle(6-Diazo-5-oxo)-OH;6-Diazo-5-oxo-L-nor-Leucine
Cas No.	157-03-9
分子式	C₆H₉N₃O₃
分子量	171.15
包装储存	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	L-6-Diazo-5-oxonorleucine (L-6-Diazo-5-oxonorleucine) 是一种谷氨酰胺拮抗剂，其Ki 值为 6 μM。L-6-Diazo-5-oxonorleucine 具有镇痛、抗菌、抗病毒和抗癌作用。L-6-Diazo-5-oxonorleucine 在体外表现出遗传毒性。L-6-Diazo-5-oxonorleucine 能降低肿瘤细胞的自我更新能力和转移能力。

生物活性

6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine; DON) is a glutamine antagonist that irreversibly inhibits the catabolic effect of glutamine. 6-Diazo-5-oxo-L-nor-Leucine shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 6-Diazo-5-oxo-L-nor-Leucine also possesses antibacterial and antiviral activity.

性状

Solid

IC50 & Target[1][2]

Bacterial.

体外研究(In Vitro)

6-Diazo-5-oxo-L-nor-Leucine (DON) (0.3 mM; 1 h) shows inhibition of glutamine catabolism in WI-L2 cells.
6-Diazo-5-oxo-L-nor-Leucine (DON) decreases the selfrenewal potential and metastatic ability of tumor cell.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	WI-L2 cells
Concentration:	0.3 mM
Incubation Time:	1 h
Result:	Inhibited the rapid catabolism of glutamine by the cultured human lymphoblast line WI-L2 greater than 95%.

体内研究(In Vivo)

6-Diazo-5-oxo-L-nor-Leucine sensitizes pancreatic tumors to anti-PD1 resulting in tumor regression and prolonged survival in vivo.
6-Diazo-5-oxo-L-nor-Leucine decreases hyaluronan and collagen in the tumor microenvironment, leading to an extensive remodeling of the ECM (extensive extracellular matrix), and an increases infiltration CD8 T-cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[1]. Willis RC, et al. The inhibition by 6-diazo-5-oxo-l-norleucine of glutamine catabolism of the cultured human lymphoblast. J Cell Physiol. 1977 Dec;93(3):375-82. [Information]

[2]. Sharma NS, et al. Targeting tumor-intrinsic hexosamine biosynthesis sensitizes pancreatic cancer to anti-PD1 therapy. J Clin Invest. 2019 Oct 15. [Information]

[3]. DeWald H A, et al. 6-diazo-5-oxo-l-norleucine, a new tumor-inhibitory substance. 1a preparation of l-, d-and dl-forms1b. Journal of the American Chemical Society, 1958, 80(15): 3941-3945.

溶解度数据

体外研究:

H₂O : 25 mg/mL (146.07 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.8428 mL	29.2141 mL	58.4283 mL
5 mM	1.1686 mL	5.8428 mL	11.6857 mL
10 mM	0.5843 mL	2.9214 mL	5.8428 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. Willis RC, et al. The inhibition by 6-diazo-5-oxo-l-norleucine of glutamine catabolism of the cultured human lymphoblast. J Cell Physiol. 1977 Dec;93(3):375-82. [Information]

[2]. Sharma NS, et al. Targeting tumor-intrinsic hexosamine biosynthesis sensitizes pancreatic cancer to anti-PD1 therapy. J Clin Invest. 2019 Oct 15. [Information]

[3]. DeWald H A, et al. 6-diazo-5-oxo-l-norleucine, a new tumor-inhibitory substance. 1a preparation of l-, d-and dl-forms1b. Journal of the American Chemical Society, 1958, 80(15): 3941-3945.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

6-diazo-5-oxo-L-nor-Leucine

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