Telaglenastat (CB-839)

For research use only.

Catalog No.S7655

47 publications

Telaglenastat (CB-839) Chemical Structure

CAS No. 1439399-58-2

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.

Selleck's Telaglenastat (CB-839) has been cited by 47 publications

Purity & Quality Control

Choose Selective Glutaminase Inhibitors

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.
Glutaminase [1]
(Cell-free assay)
24 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 cells NVnpPWdZS3m2b4TvfIlkcXS7IHHzd4F6 NWrtUJdiPiCmYYnz MoXTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDt[YF{fXKnZDDvckA3fGhiZHH5JIJ6KGinbX;jfZRwdWW2comsJGlEPTB;MD6wN|Mh|ryP NHuyUIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm4PFgxOyd-Mk[5PFg5ODN:L3G+
TNBC cell lines M2TzW2dzd3e2aDDpcohq[mm2b36gZZN{[Xl? MlLTNUDPxE1? NVf5dFRMPCCmYYnz NIXJfXVESi16M{mgeJJm[XSvZX70JIlv\HWlZXSgZ4VtdCCub4PzJI9zKGSnY4LlZZNm\CClZXzsJJBzd2yrZnXyZZRqd25iYomgcY9z\SC2aHHuJFUxLSCrbjDzbZgh[2WubDDsbY5meyBqSFPDNVgxPixiSFPDNVE1OyxiSFPDN|gtKE2GQT3NRk01OzZuIF3ERU1OSi1{M{GgZY5lKEi|NUe4WEk8KHSqZTDveIhmeiC|aYigZ4VtdCCuaX7ld{ApUEOFMUmzO{whUEOFN{CsJGJVPTR7LDDNSGEuVUJvMUW3MEBOTEFvTVKtOFU{KGGwZDDNSGEuVUJ2NkipJJdmemViZXn0bIVzKG6xdDDh[oZm[3SnZDDvdkBp[WRidHjlbZIh[2WubDDwdo9tcW[ncnH0bY9vKGGoZnXjeIVlKGK7IHzld5MhfGijbjC1NEUh[W6mIIfldoUh[2GubHXkJJJme2m|dHHueE4> NVX2T3QzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwOFAyQDFpPkOxNFQxOThzPD;hQi=>
MM.1S BzR cells MofmSpVv[3Srb36gZZN{[Xl? NGn4[ZY2KM7:TR?= M{W5[lE3KGixdYLz M1PZeJRz\WG2bXXueEB4cXSqIFPCMVg{QSC|aXfubYZq[2GwdHz5JJJmeHKnc4Pl[EBwgHmpZX6gZ49ve3WvcITpc44hemG2ZTDpckBxem:2ZXHzc41mNWmwaHnibZRweiC{ZYPpd5RidnRiY3XscJMv MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDRzNUe4Nkc,Ojh2MUW3PFI9N2F-
MM.1S cells MYnD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M2r5SFczKGixdYLz Mn\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2MUW3PFIoRjJ6NEG1O|gzRC:jPh?=
U266 cell lines NGOyZZBE\WyuII\pZYJqdGm2eTDhd5NigQ>? NHTTfng4OiCqb4Xydy=> NWHmSJltRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0NVU4QDJpPkK4OFE2Pzh{PD;hQi=>
HT1080 NE\DV3VEgXSxdH;4bYNqfHliYYPzZZk> MoHtOFghcA>? MXXJR|UxKD1iNESuN|gh|ryP MkXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzN{SxNFUoRjJ6MUe0NVA2RC:jPh?=
HCC827 MlXFR5l1d3SxeHnjbZR6KGG|c3H5 MY\JR|UxKD1iNUGuOFIh|ryP MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF5NEGwOUc,OjhzN{SxNFU9N2F-

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
collagen I/collagen III; 

PubMed: 29019707     

Idiopathic pulmonary fibrosis lung fibroblasts were treated with or without 1 μM CB-839 for 48 hours. The amounts of indicated proteins were determined by Western blotting. 

Growth inhibition assay
Cell growth; 

PubMed: 28967864     

Proliferation of various KEAP1 wild type human cancer cell lines. Cells were pretreated with 1 μM KI696 where indicated followed by 250 nM CB-839 treatment for 5 days. All data is presented as relative to the untreated condition for each cell line (n = 3, triplicate wells). All error bars depict s.e.m. ****p<0.0001.

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]


Kinase Assay:


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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:


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  • 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.

    (Only for Reference)
Animal Research:


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  • Animal Models: Female Scid/Bg mice bearing TNBC or JIMT-1 xenograft
  • Dosages: 200 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (174.95 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.

* 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.

Chemical Information

Molecular Weight 571.57


CAS No. 1439399-58-2
Storage powder
in solvent
Synonyms N/A
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

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04250545 Recruiting Drug: Sapanisertib|Drug: Telaglenastat Hydrochloride 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) November 9 2020 Phase 1
NCT03875313 Terminated Drug: CB-839|Drug: Talazoparib Solid Tumor|Clear Cell Renal Cell Carcinoma|TNBC - Triple-Negative Breast Cancer|Colorectal Cancer|CRC|RCC|ccRCC Calithera Biosciences Inc May 20 2019 Phase 1|Phase 2
NCT02944435 Completed Drug: CB-839 Capsules|Drug: CB-839 Tablets Healthy Volunteers Calithera Biosciences Inc October 2016 Phase 1
NCT02771626 Completed Drug: CB-839|Drug: Nivolumab Clear Cell Renal Cell Carcinoma (ccRCC)|Melanoma|Non-small Cell Lung Cancer (NSCLC) Calithera Biosciences Inc August 1 2016 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID