1. Autophagy
    Metabolic Enzyme/Protease
  2. Autophagy
    Glutaminase
  3. Telaglenastat

Telaglenastat (Synonyms: CB-839)

Cat. No.: HY-12248 Purity: 99.92%
Handling Instructions

Telaglenastat (CB-839) is a potent, selective, and orally bioavailable inhibitor of glutaminase (KGA and GAC) with IC50s of 28 and 23 nM for glutaminase in kidney and brain.

For research use only. We do not sell to patients.

Telaglenastat Chemical Structure

Telaglenastat Chemical Structure

CAS No. : 1439399-58-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 75 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 270 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 20 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Telaglenastat purchased from MCE. Usage Cited in: Am J Respir Cell Mol Biol. 2018 Mar;58(3):378-390.

    Human normal lung fibroblasts are treated as in A. Levels of the indicated proteins are determined by Western blotting. CB-839 remarkably inhibits the expression of Collagens I and III in myofibroblasts.

    Telaglenastat purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Oct 2;504(2):415-421.

    PC3 cells are treated with indicated doses of CB-839 for 24 h after c-Myc overexpression. Cells are then harvested for the determination of indicated proteins levels.

    Telaglenastat purchased from MCE. Usage Cited in: Blood Adv. 2017 Jul 14;1(17):1296-1305.

    The drug could be detected through MS only in the plasma from rats receiving its administration, confirming its systemic bioavailability after the treatment. Labeling scheme in panels B and C is based on the presence (+) or absence (−) of shock, DMSO (control for vehicle to the drug CB-839), and glutaminase inhibitor. Three columns are graphed per each group, indicating baseline, postshock, and end-of-shock values.

    Telaglenastat purchased from MCE. Usage Cited in: Cancer Discov. 2017 Apr;7(4):380-390.

    MEFs treated with 12.5 nM CB-839 or control (one-way ANOVA).

    Telaglenastat purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 Jun;40(6):814-822.

    The protein expression levels of the genes related to cell cycle and metabolism are detected by immunoblotting using the corresponding antibodies in H1299 cells treated with 20 nM THZ1 alone or in combination with 500 nM CB-839 for 48 h.
    • Biological Activity

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    • Customer Review

    Description

    Telaglenastat (CB-839) is a potent, selective, and orally bioavailable inhibitor of glutaminase (KGA and GAC) with IC50s of 28 and 23 nM for glutaminase in kidney and brain[1].

    IC50 & Target

    IC50: 23 nM (glutaminase in kindey), 28 nM (glutaminase in brain)[1]

    In Vitro

    Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s of 49 nM and 26 nM, respectively[1].
    Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells[1].

    Cell Proliferation Assay[1]

    Cell Line: HCC1806, MDA-MB-231 cells
    Concentration: 0.1, 1, 10, 100, 1000 nM
    Incubation Time: 72 hours
    Result: Has a potent effect on the proliferation of the two TNBC cell lines (IC50 of 49 nM and 26 nM for HCC1806 and MDA-MB-231 cells).

    Apoptosis Analysis[1]

    Cell Line: MDA-MB-231, HCC1806 cells
    Concentration: 1 μM
    Incubation Time: 72 hours
    Result: Caspase 3/7 activation.
    In Vivo

    Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1].

    Animal Model: Female nu/nu mice with age 4–6 weeks (TNBC patient-derived xenograft model)[1]
    Dosage: 200 mg/kg
    Administration: Oral administration; twice daily for 28 days
    Result: Suppressed tumor growth by 61% relative to vehicle control at the end of study.
    Molecular Weight

    571.57

    Formula

    C₂₆H₂₄F₃N₇O₃S

    CAS No.

    1439399-58-2

    SMILES

    O=C(NC1=NN=C(CCCCC2=NN=C(NC(CC3=CC=CC(OC(F)(F)F)=C3)=O)C=C2)S1)CC4=NC=CC=C4

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (52.49 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7496 mL 8.7478 mL 17.4957 mL
    5 mM 0.3499 mL 1.7496 mL 3.4991 mL
    10 mM 0.1750 mL 0.8748 mL 1.7496 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.08 mg/mL (3.64 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (3.64 mM); Clear solution

    • 3.

      Add each solvent one by one:  20% HP-β-CD/10 mM citrate pH 2.0

      Solubility: 1 mg/mL (1.75 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.92%

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    Product Name:
    Telaglenastat
    Cat. No.:
    HY-12248
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