CB 839

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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