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6-Diazo-5-oxo-L-nor-Leucine

Name: 6-Diazo-5-oxo-L-nor-Leucine
Brand: TargetMol
SKU: T8373
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: L-6-Diazo-5-oxonorleucine, DON, Diazooxonorleucine) Copy Product Info

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Synonyms: L-6-Diazo-5-oxonorleucine, DON, Diazooxonorleucine

Catalog No. T8373 Copy Product Info

Purity: 98.93%

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6-Diazo-5-oxo-L-nor-Leucine (DON) is a glutamine antagonist, an irreversible glutaminolysis inhibitor (Ki=6 μM) with antitumor (particularly pancreatic cancer), antibacterial, and antiviral activities.

Cas No. 157-03-9

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Pack Size	Price	USA Stock	Global Stock
1 mg	$40	In Stock	In Stock
5 mg	$123	In Stock	In Stock
10 mg	$183	In Stock	In Stock
25 mg	$297	In Stock	In Stock
50 mg	$456	In Stock	In Stock
100 mg	$668	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$80	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.93%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	6-Diazo-5-oxo-L-nor-Leucine (DON) is a glutamine antagonist, an irreversible glutaminolysis inhibitor (Ki=6 μM) with antitumor (particularly pancreatic cancer), antibacterial, and antiviral activities.
Targets & IC50	GLS1:~1 mM, Glutaminases:6 μM (Ki)
In vitro	Methods: Thyroid cancer TPC-1, K1, BCPAP, FTC133, and 8305C cells were used to evaluate 6-Diazo-5-oxo-L-nor-Leucine in vitro activity through CCK-8, EdU incorporation, and colony formation assays. Cells were treated at concentrations of 0.5–2.0 μmol/L for 48–72 hours or 5–10 days. Results: The compound concentration-dependently inhibited cell viability, DNA synthesis, and colony formation, induced S phase arrest, and downregulated cell cycle-related proteins including CDK2 and Cyclin A.[1] Methods: U251, U87, and SF767 glioblastoma cells were used to evaluate 6-Diazo-5-oxo-L-nor-Leucine in vitro activity through MTS cell proliferation assay. Cells were treated with increasing concentrations of 6-Diazo-5-oxo-L-nor-Leucine for 72 hours. Results: The compound dose-dependently inhibited proliferation of the above cell lines, and showed synergistic enhancement when combined with L-asparaginase.[2] Methods: C4-2/MDVR castration-resistant prostate cancer cells were used to validate 6-Diazo-5-oxo-L-nor-Leucine in vitro activity through metabolic profiling and isotope tracing experiments. Cells were treated at 5 μmol/L concentration for 48 hours. Results: The compound significantly increased intracellular glutamine levels, reduced tricarboxylic acid cycle intermediates and nucleotide metabolites, while blocking glutamine carbon metabolism and nitrogen metabolism pathways.[3]
In vivo	Methods: A K1 thyroid cancer xenograft model was established by subcutaneous transplantation in BALB/c nude mice. The prodrug of 6-Diazo-5-oxo-L-nor-Leucine, JHU-083 (2 mg/kg), was administered every other day, initially by oral gavage and subsequently by intraperitoneal injection, with PBS as the control. Results: JHU-083 significantly inhibited tumor growth, reduced tumor weight, decreased Ki-67-positive cells, and caused no obvious toxicity, confirming the in vivo antitumor activity of 6-Diazo-5-oxo-L-nor-Leucine. [1] Methods: A U87 human glioma xenograft model was established by subcutaneous transplantation in female athymic mice. 6-Diazo-5-oxo-L-nor-Leucine was administered by intraperitoneal injection at a dose of 0.8 mg/kg once daily for 6 consecutive days, with HEPES-buffered saline as the vehicle; the control group received an equal volume of vehicle. Results: 6-Diazo-5-oxo-L-nor-Leucine significantly inhibited tumor growth compared to the control group, with statistical significance. [4]
Synonyms	L-6-Diazo-5-oxonorleucine, DON, Diazooxonorleucine

Chemical Properties

Molecular Weight	171.15
Formula	C₆H₉N₃O₃
Cas No.	157-03-9
Smiles	N[C@@H](CCC(=O)C=[N+]=[N-])C(O)=O
Relative Density.	1.3994 g/cm3 (Estimated)

Storage & Solubility Information

Storage

Store at low temperature,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 7 mg/mL (40.9 mM), Sonication is recommended.

H2O: 12.5 mg/mL (73.04 mM), Sonication is recommended.

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	5.8428 mL	29.2141 mL	58.4283 mL	292.1414 mL
5 mM	1.1686 mL	5.8428 mL	11.6857 mL	58.4283 mL
10 mM	0.5843 mL	2.9214 mL	5.8428 mL	29.2141 mL
20 mM	0.2921 mL	1.4607 mL	2.9214 mL	14.6071 mL

H2O

	1mg	5mg	10mg	50mg
50 mM	0.1169 mL	0.5843 mL	1.1686 mL	5.8428 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

InhibitorinhibitInfluenzaVirusInfluenza VirusGlutaminaseBacterialAntibiotic6-Diazo-5-oxo-L-nor-Leucine6Diazo5oxoLnorLeucine6 Diazo 5 oxo L nor Leucine

Related Tags: 6-Diazo-5-oxo-L-nor-Leucine chemical structure | 6-Diazo-5-oxo-L-nor-Leucine in vivo | 6-Diazo-5-oxo-L-nor-Leucine in vitro | 6-Diazo-5-oxo-L-nor-Leucine formula | 6-Diazo-5-oxo-L-nor-Leucine molecular weight