CB-839

Catalog No.S7655

CB-839 Chemical Structure

Molecular Weight(MW): 571.57

CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.

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1 Customer Review

  • Combination treatment with a GLS1 inhibitor and PP242 induces cell death. a The SKOV3 and A2780 cells were incubated with DMSO (control), PP242 (1 μM), CB839 (1 μM), or their combination for 48 h. Cell morphology images were obtained under a microscope. b. Expression of the activated cleaved PARP content to GAPDH was observed using Western blot. c. Cell death was evaluated by flow cytometry after Annexin V and PI staining. Data are presented as means of triplicate samples, and error bars reflect SD.

    Tumor Biol, 2016, 37:11007-11015.. CB-839 purchased from Selleck.

Purity & Quality Control

Choose Selective Glutaminase Inhibitors

Biological Activity

Description CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.
Targets
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]

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]

Protocol

Kinase Assay:[1]
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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:[1]
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  • Cell lines: HCC1806, MDA-MB-231, and T47D cells
  • Concentrations: 1 mM
  • 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:[1]
+ Expand
  • Animal Models: Female Scid/Bg mice bearing TNBC or JIMT-1 xenograft
  • Formulation: 25% (w/v) hydroxypropyl-b-cyclodextrin (HPBCD) in 10 mmol/L citrate, pH 2
  • 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:
5% DMSO+corn oil
3mg/mL

* 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
Formula

 C26H24F3N7O3S

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02944435 Completed Healthy Volunteers Calithera Biosciences, Inc October 2016 Phase 1
NCT02861300 Recruiting Colorectal Cancer|Colon Cancer|Rectal Cancer|Solid Tumor Case Comprehensive Cancer Center August 2016 Phase 1|Phase 2
NCT02771626 Recruiting Clear Cell Renal Cell Carcinoma|Melanoma|Non-small Cell Lung Cancer Calithera Biosciences, Inc August 2016 Phase 1|Phase 2
NCT02071927 Completed Acute Myeloid Leukemia (AML)|Acute Lymphocytic Leukemia (ALL) Calithera Biosciences, Inc March 2014 Phase 1
NCT02071888 Completed Non-Hodgkins Lymphoma (NHL)|Multiple Myeloma|Waldenstroms Macroglobulinemia (WM)|Diffuse Large B-cell Lymphoma (DLBCL),|Other B-cell NHL Subtypes, Including WM|T-cell NHL Calithera Biosciences, Inc February 2014 Phase 1
NCT02071862 Recruiting Solid Tumors|Triple-Negative Breast Cancer|Non Small Cell Lung Cancer|Renal Cell Carcinoma|Mesothelioma|Fumarate Hydratase (FH)-Deficient Tumors|Succinate Dehydrogenase (SDH)-Deficient Gastrointestinal Stromal Tumors (GIST)|Succinate Dehydrogenase (SDH)-Deficient Non-gastrointestinal Stromal Tumors|Tumors Harboring Isocitrate Dehydrogenase-1 (IDH1) and IDH2 Mutations|Tumors Harboring Amplifications in the cMyc Gene Calithera Biosciences, Inc February 2014 Phase 1

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID