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CB 839 New
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
|Storage||Store at -20°C|
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 Data for CB 839
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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||17.5 mL|
|5 mM||0.35 mL||1.75 mL||3.5 mL|
|10 mM||0.17 mL||0.87 mL||1.75 mL|
|50 mM||0.03 mL||0.17 mL||0.35 mL|
References for CB 839
References are publications that support the biological activity of the product.
Gross et al (2014) Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol.Cancer Ther. 13 890 PMID: 24523301
Jacque et al (2015) Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition. Blood 126 1346 PMID: 26186940
Matre et al (2016) Inhibiting glutaminase in acute myeloid leukemia: metabolic dependency of selected AML subtypes. Oncotarget 7 79722 PMID: 27806325
Momcilovic et al (2017) Targeted inhibition of EGFR and glutaminase induces metabolic crisis in EGFR mutant lung cancer. Cell Rep. 18 601 PMID: 28099841
Biancur et al (2017) Compensatory metabolic networks in pancreatic cancers upon perturbation of glutamine metabolism. Nat.Commun. 8 15965 PMID: 28671190
Zhou et al (2019) Estrogen inhibits autophagy and promotes growth of endometrial cancer by promoting glutamine metabolism. Cell Commun.Signal. 17 99 PMID: 31429768
If you know of a relevant reference for CB 839, please let us know.
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Citations for CB 839
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Literature in this Area
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Cancer Metabolism Poster
Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.