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Formula | C26H24F3N7O3S |
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Molecular Weight | 571.57 | CAS No. | 1439399-58-2 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (174.95 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1. | ||
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In vitro | CB-839 exhibits time-dependent and slowly reversible kinetics. IC50 values for glutaminase inhibition by CB-839 following preincubation with rHu-GAC for-1 hour are < 50 nmol/L, at least 13-fold lower than with BPTES. CB-839 has antiproliferative activity in a triple-negative breast cancer (TNBC) cell line, HCC-1806, while no antiproliferative activity is observed in an estrogen receptor–positive cell line, T47D.[1] |
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In vivo | In the mouse TNBC model, single agent CB-839 (200 mg/kg, p.o.) suppresses tumor growth by 61% relative to vehicle control. In the mouse JIMT-1 xenograft model, CB-839 alone (200 mg/kg, p.o.) results in 54% tumor growth inhibition (TGI) relative to vehicle control, combination of CB-839 (200 mg/kg, p.o.) with NSC 125973(10 mg/kg, p.o.) largely suppresses the regrowth of the tumors resulting in a TGI relative to vehicle control of 100%.[1] |
Kinase Assay: |
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Cell Assay: |
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Animal Study: |
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Data from [Data independently produced by , , Haematologica, 2018, doi:10.3324/haematol.2018.204701]
Data from [Data independently produced by , , Br J Cancer, 2018, 118(8):1074-1083]
Data from [Data independently produced by , , Biochem Pharmacol, 2018, 156:204-214]
Data from [Data independently produced by , , Tumor Biol, 2016, 37:11007-11015.]
Succinate dehydrogenase deficiency-driven succinate accumulation induces drug resistance in acute myeloid leukemia via ubiquitin-cullin regulation [ Nat Commun, 2024, 15(1):9820] | PubMed: 39537588 |
HuR controls glutaminase RNA metabolism [ Nat Commun, 2024, 15(1):5620] | PubMed: 38965208 |
A personalized medicine approach identifies enasidenib as an efficient treatment for IDH2 mutant chondrosarcoma [ EBioMedicine, 2024, 102:105090] | PubMed: 38547578 |
Small molecules targeting selective PCK1 and PGC-1α lysine acetylation cause anti-diabetic action through increased lactate oxidation [ Cell Chem Biol, 2024, 31(10):1772-1786.e5] | PubMed: 39341205 |
Targeting the glutamine metabolism to suppress cell proliferation in mesenchymal docetaxel-resistant prostate cancer [ Oncogene, 2024, 43(26):2038-2050] | PubMed: 38750263 |
Targeting metabolic adaptive responses induced by glucose starvation inhibits cell proliferation and enhances cell death in osimertinib-resistant non-small cell lung cancer (NSCLC) cell lines [ Biochem Pharmacol, 2024, S0006-2952(24)00144-8] | PubMed: 38522556 |
ERK5 Interacts with Mitochondrial Glutaminase and Regulates Its Expression [ Int J Mol Sci, 2024, 25(6)3273] | PubMed: 38542254 |
Prostate Cancer's Silent Partners: Fibroblasts and Their Influence on Glutamine Metabolism Manipulation [ Int J Mol Sci, 2024, 25(17)9275] | PubMed: 39273225 |
Mesenchymal Stem Cells Promote an Increase in Neuronal Oscillation via Glutamate Tonic Release [ Neuroscience, 2024, 552:76-88] | PubMed: 38909673 |
Glutaminase 1 plays critical roles in myelodysplastic syndrome and acute myeloid leukemia cells [ Cancer Biomark, 2024, 41(1):55-68] | PubMed: 39213050 |
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