CB 839

Name: CB 839
Brand: Tocris Bioscience
SKU: 7591

Tocris Bioscience, part of Bio-Techne | Catalog # 7591

Citations (7)

COA / SDS

Potent glutaminase GLS1 inhibitor

Key Product Details

Description:	Potent glutaminase GLS1 inhibitor
Chemical Name:	N-[5-[4-[6-[[2-[3-(Trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-2-pyridineacetamide
Purity:	≥98% (HPLC)
Molecular Weight:	571.58

View Full Technical Details for CB 839

Technical Data
Citations

Biological Activity for CB 839

CB 839 is a potent non-competitive glutaminase (GLS1) inhibitor (IC₅₀ = 24 nM for recombinant human GAC). The compound exhibits selectivity for GLS1 over GLS2. CB 839 displays antiproliferative activity in a triple-negative breast cancer cell line (GI₅₀ values are 19 and 55 nM against MDA-MB-231 and HCC1806, respectively); it reduces glutamine consumption and glutamate production rates in HCC1806 cells. CB 839 displays significant antitumor activity as a single agent in a patient-derived TNBC xenografts model. CB 839 inhibits the growth of basal-like HER2 cell line JIMT-1 xenografts in mice, both as a single agent and in combination with Paclitaxel (Cat. No. 1097). CB 839 works with Erlotinib (Cat. No. 7194) to reduce glucose and glutamine uptake, increase energetic stress and activate the AMP-activated protein kinase (AMPK) pathway in EGFR (del19) non-small cell lung cancer xenografts in vivo. CB 839 is orally bioavailable.

Technical Data for CB 839

M. Wt	571.58
Formula	C₂₆H₂₄F₃N₇O₃S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1439399-58-2
PubChem ID	71577426
InChi Key	PRAAPINBUWJLGA-UHFFFAOYSA-N
Smiles	O=C(NC1=NN=C(CCCCC2=NN=C(NC(CC3=CC=CC(OC(F)(F)F)=C3)=O)C=C2)S1)CC4=NC=CC=C4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for CB 839

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	57.16	100

Preparing Stock Solutions for CB 839

The following data is based on the product molecular weight 571.58.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.75 mL	8.75 mL	17.50 mL
5 mM	0.35 mL	1.75 mL	3.50 mL
10 mM	0.17 mL	0.87 mL	1.75 mL
50 mM	0.03 mL	0.17 mL	0.35 mL

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References for CB 839

References are publications that support the biological activity of the product.

Zhou Estrogen inhibits autophagy and promotes growth of endometrial cancer by promoting glutamine metabolism. Cell Commun.Signal. 2019 PMID: 31429768
Biancur Compensatory metabolic networks in pancreatic cancers upon perturbation of glutamine metabolism. Nat.Commun. 2017 PMID: 28671190
Momcilovic Targeted inhibition of EGFR and glutaminase induces metabolic crisis in EGFR mutant lung cancer. Cell Rep. 2017 PMID: 28099841
Matre Inhibiting glutaminase in acute myeloid leukemia: metabolic dependency of selected AML subtypes. Oncotarget 2016 PMID: 27806325
Jacque Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition. Blood 2015 PMID: 26186940
Gross Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol.Cancer Ther. 2014 PMID: 24523301