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

Telaglenastat hydrochloride (Synonyms: CB-839 hydrochloride)

Cat. No.: HY-12248A
Handling Instructions

Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity.

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

Telaglenastat hydrochloride Chemical Structure

Telaglenastat hydrochloride Chemical Structure

CAS No. : 1874231-60-3

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Top Publications Citing Use of Products

    Telaglenastat hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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.
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    Description

    Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity[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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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

    608.04

    Formula

    C₂₆H₂₅ClF₃N₇O₃S

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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