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

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10mg

￥1304.00

650.00

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25mg

￥2959.00

1500.00

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50mg

￥5306.00

2800.00

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1g

￥30000.00

0.00

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6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine; DON) 是一种谷氨酰胺拮抗剂，能不可逆地抑制谷氨酰胺的分解作用。6-Diazo-5-oxo-L-nor-Leucine 具有较好的抗癌活性 (尤其是胰腺癌)，能降低肿瘤细胞的自我更新潜力和转移能力。6-Diazo-5-oxo-L-nor-Leucine 还具有抗菌和抗病毒活性。

货号：ajci66690
CAS：157-03-9
别名：6-重氮-5-氧代-L-正亮氨酸; L-6-Diazo-5-oxonorleucine; DON
分子式：C6H9N3O3
分子量：171.2
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1][2][3].

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.

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

[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.

Protocol

Cell experiment [1]:
Cell lines	MC38 cells
Preparation Method	Tumor cells treated with increasing concentrations of 6-Diazo-5-oxo-L-nor-Leucine for 48h.
Reaction Conditions	10^-2µM-10²µM ;48h
Applications	6-Diazo-5-oxo-L-nor-Leucine inhibited cell proliferation, and the inhibitory effect increased with the increase of concentration.
Animal experiment [2]:
Animal models	Female athymic nude (nu/J) mice (pancreatic cancer cells S2VP10)
Preparation Method	The tumors reached a size of 100 mm and were given to 6-Diazo-5-oxo-L-nor-Leucine at the end of the 4th week, and the mice were killed.
Dosage form	1 mg/kg;5 days a week
Applications	Treatment with 6-Diazo-5-oxo-L-nor-Leucine decreased tumor progression as well as end-of-study tumor weight and volume.
References: [1]. Leone RD, Zhao L, et,al. Glutamine blockade induces divergent metabolic programs to overcome tumor immune evasion. Science. 2019 Nov 22;366(6468):1013-1021. doi: 10.1126/science.aav2588. Epub 2019 Nov 7. PMID: 31699883; PMCID: PMC7023461. [2].Sharma NS, Gupta VK, et,al. Targeting tumor-intrinsic hexosamine biosynthesis sensitizes pancreatic cancer to anti-PD1 therapy. J Clin Invest. 2020 Jan 2;130(1):451-465. doi: 10.1172/JCI127515. PMID: 31613799; PMCID: PMC6934212.