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Telaglenastat hydrochloride

Catalog No. T39309 CAS 1874231-60-3

Synonyms: CB-839 hydrochloride

Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1). It selectively inhibits the splice variants of GLS1, specifically KGA (kidney-type glutaminase) and GAC (glutaminase C), as compared to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain. In addition, it induces autophagy and exhibits antitumor activity.

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Telaglenastat hydrochloride Chemical Structure

Telaglenastat hydrochloride, CAS 1874231-60-3

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Biological Description

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Description	Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1). It selectively inhibits the splice variants of GLS1, specifically KGA (kidney-type glutaminase) and GAC (glutaminase C), as compared to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain. In addition, it induces autophagy and exhibits antitumor activity.
In vitro	Telaglenastat (CB-839), administered at concentrations ranging from 0.1 to 1000 nM for a period of 72 hours, exhibits significant antiproliferative effects on HCC1806 and MDA-MB-231 cell lines, with IC50 values of 49 nM and 26 nM, respectively. Furthermore, at a concentration of 1 μM over the same duration, Telaglenastat activates caspase 3/7 and triggers apoptosis in these cell lines. The findings from the Cell Proliferation Assay and Apoptosis Analysis highlight Telaglenastat's capability to effectively inhibit cell growth and induce apoptosis in TNBC (triple-negative breast cancer) cells, marking its potential in cancer treatment strategies.
In vivo	Telaglenastat (CB-839) demonstrated antitumor activity in TNBC xenograft models, achieving a 61% suppression of tumor growth relative to vehicle control after twice-daily oral administration (200 mg/kg) for 28 days in female nu/nu mice aged 4-6 weeks. The mice were part of a TNBC patient-derived xenograft model[1].

Synonyms	CB-839 hydrochloride
Molecular Weight	608.04
Formula	C26H25ClF3N7O3S
CAS No.	1874231-60-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Gross MI, et al. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901. 2. Biancur DE, et al. Compensatory metabolic networks in pancreatic cancers upon perturbation of glutaminemetabolism. Nat Commun. 2017 Jul 3;8:15965. 3. Zhou WJ, et al. Estrogen inhibits autophagy and promotes growth of endometrial cancer by promoting glutamine metabolism. Cell Commun Signal. 2019 Aug 20;17(1):99.

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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.

Keywords

Telaglenastat hydrochloride 1874231-60-3 CB-839 hydrochloride CB 839 Hydrochloride Telaglenastat Hydrochloride CB839 Hydrochloride CB-839 Hydrochloride inhibitor inhibit

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