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Glutaminase-IN-1

Name: Glutaminase-IN-1
Brand: TargetMol
SKU: T11421
Price: 42 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11421Cas No. 2247127-79-1

Alias CB839 derivative

Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine inhibitor of the renal-type glutaminase (KGA) variant, exhibited antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model.

Glutaminase-IN-1

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Purity: 98.65%

Catalog No. T11421Alias CB839 derivativeCas No. 2247127-79-1

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$42	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.65%

Appearance:Solid

Color:Yellow

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COA LCMS

Product Introduction

Bioactivity

Description	Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine inhibitor of the renal-type glutaminase (KGA) variant, exhibited antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model.
Targets&IC50	A549 cells:17 nM, HCT116 cells:9 nM, Caki-1 cells:19 nM, H2:6.78 μM, KGA:1 nM
In vitro	Glutaminase-IN-1 (CPD20) is a derivative of CB839, serving as a conformational inhibitor of kidney-type glutaminase (KGA) with an IC50 of 1 nM. Glutaminase-IN-1 exhibits improved cellular uptake and anti-tumor activity. The IC50 values of Glutaminase-IN-1 in A549, H2, Caki-1, and HCT116 cell lines are 17 nM, 6.78 μM, 19 nM, and 9 nM, respectively. Glutaminase-IN-1 demonstrates superior KGA inhibitory activity compared to the corresponding BPTES and CB839[1].
In vivo	Glutaminase-IN-1 (10 mg/kg, subcutaneous) reduced the size and weight of HCT116 tumors, and statistical analysis indicated a significant 40% reduction in tumor weight with CPD20. Glutaminase-IN-1 significantly prolonged the survival of mice carrying H22[1].
Synonyms	CB839 derivative

Chemical Properties

Molecular Weight	618.47
Formula	C₂₆H₂₄F₃N₇O₃Se
Cas No.	2247127-79-1
Smiles	C(C(NC1=CC=C(CCCCC=2[Se]C(NC(CC3=CC=CC=N3)=O)=NN2)N=N1)=O)C4=CC(OC(F)(F)F)=CC=C4
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (161.69 mM), Sonication is recommended.

H2O: 1 mg/mL (1.62 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.34 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6169 mL	8.0845 mL	16.1689 mL	80.8447 mL

DMSO

	1mg	5mg	10mg	50mg
5 mM	0.3234 mL	1.6169 mL	3.2338 mL	16.1689 mL
10 mM	0.1617 mL	0.8084 mL	1.6169 mL	8.0845 mL
20 mM	0.0808 mL	0.4042 mL	0.8084 mL	4.0422 mL
50 mM	0.0323 mL	0.1617 mL	0.3234 mL	1.6169 mL
100 mM	0.0162 mL	0.0808 mL	0.1617 mL	0.8084 mL

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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