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Glutaminase-IN-1

Name: Glutaminase-IN-1
Brand: TargetMol
SKU: T11421
Price: 39 EUR
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	Availability	Quantity
1 mg	39 €	In Stock

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Purity:98.65%

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COA LCMS

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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, H2:6.78 μM, Caki-1 cells:19 nM, 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].
Alias	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.

Solubility Information

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

H2O: 1 mg/mL (1.61 mM), Sonication is recommended.

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 mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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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