Home Proteases Glutaminase inhibitor - Autophagy activator Telaglenastat (CB-839) For research use only.

Telaglenastat (CB-839)

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.

Telaglenastat (CB-839) Chemical Structure

Telaglenastat (CB-839) Chemical Structure

CAS: 1439399-58-2

Selleck's Telaglenastat (CB-839) has been cited by 86 publications

Purity & Quality Control

Batch: Purity: 99.95%
99.95

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Choose Selective Glutaminase Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 cells Cytotoxicity assay 6 days Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry, IC50=0.033 μM 26988803
TNBC cell lines Growth inhibiton assay 1 μM 4 days CB-839 treatment induced cell loss or decreased cell proliferation by more than 50% in six cell lines (HCC1806, HCC1143, HCC38, MDA-MB-436, MDA-MB-231 and Hs578T); the other six cell lines (HCC1937, HCC70, BT549, MDA-MB-157, MDA-MB-453 and MDA-MB468) were either not affected or had their cell proliferation affected by less than 50% and were called resistant. 31040181
MM.1S BzR cells Function assay 5 μM 16 hours treatment with CB-839 significantly repressed oxygen consumption rate in proteasome-inhibitor resistant cells. 28415782
MM.1S cells Cell viability assay 72 hours 28415782
U266 cell lines Cell viability assay 72 hours 28415782
HT1080 Cytotoxicity assay 48 h IC50 = 44.38 μM 28174105
HCC827 Cytotoxicity assay IC50 = 51.42 μM 28174105
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Biological Activity

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.
Targets
Glutaminase [1]
(Cell-free assay)
24 nM
In vitro
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]
Kinase Assay Inhibition of CB-839 on rHu-GAC
The enzymatic activity is measured in assay buffer containing 50 mM Tris-Acetate pH 8.6, 150 mM K2HPO4 , 0.25 mM EDTA, 0.1 mg/mL bovine serum albumin, 1 mM DTT, 2 mM NADP+ and 0.01% Triton X-100. To measure inhibition, the inhibitor (prepared in DMSO) is first pre-mixed with glutamine and glutamate dehydrogenase (GDH) and reactions are initiated by the addition of rHu-GAC. Final reactions contains 2 nM rHu-GAC, 10 mM glutamine, 6 units/mL GDH and 2% DMSO. Generation of NADPH is monitored by fluorescence (Ex340/Em460 nm) every minute for 15 minutes on a SpectraMax M5e plate reader. Relative fluorescence units (RFU) are converted to units of NADPH concentration (µM) using a standard curve of NADPH. Each assay plate incorporates control reactions that monitores the conversion of glutamate (1 to 75 µM) plus NADP+ to α-ketoglutarate plus NADPH by GDH. Under these assay conditions, up to 75 µM glutamate is stoichiometrically converts to α-ketoglutarate/NADPH by GDH. Initial reaction velocities are calculated by fitting the first 5 minutes of each progress curve to a straight line. Inhibition curves are fitted to a four-parameter dose response equation of the form: % activity = Bottom + (Top-Bottom)/(1+10^((LogIC50-X)*HillSlope)).
Cell Research Cell lines HCC1806, MDA-MB-231, and T47D cells
Concentrations 0.1-1000 nM
Incubation Time 72 h
Method

For viability assays, all cell lines are treated with CB-839 at the indicated concentrations for 72 hours and analyzed for antiproliferative effects using Cell Titer Glo.
Experimental Result Images Methods Biomarkers Images PMID
Western blot collagen I/collagen III 29019707
Growth inhibition assay Cell growth 28967864
In Vivo
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 paclitaxel (10 mg/kg, p.o.) largely suppresses the regrowth of the tumors resulting in a TGI relative to vehicle control of 100%.[1]
Animal Research Animal Models Female Scid/Bg mice bearing TNBC or JIMT-1 xenograft
Dosages 200 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04250545 Suspended Leptomeningeal Neoplasm|Metastatic Lung Non-Small Cell Carcinoma|Metastatic Malignant Neoplasm in the Brain|Recurrent Lung Non-Small Cell Carcinoma|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8 National Cancer Institute (NCI) October 26 2020 Phase 1
NCT02944435 Completed Healthy Volunteers Calithera Biosciences Inc October 2016 Phase 1
NCT02071927 Completed Acute Myeloid Leukemia (AML)|Acute Lymphocytic Leukemia (ALL) Calithera Biosciences Inc March 2014 Phase 1

Chemical lnformation & Solubility

Molecular Weight 571.57 Formula

 C26H24F3N7O3S
CAS No. 1439399-58-2 SDF Download Telaglenastat (CB-839) SDF
Smiles C1=CC=NC(=C1)CC(=O)NC2=NN=C(S2)CCCCC3=NN=C(C=C3)NC(=O)CC4=CC(=CC=C4)OC(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (174.95 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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