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

Telaglenastat hydrochloride  (Synonyms: CB-839 hydrochloride)

Cat. No.: HY-12248A Purity: 98.03%
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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.

CAS No. : 1874231-60-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 104 publication(s) in Google Scholar

Other Forms of Telaglenastat hydrochloride:

Telaglenastat hydrochloride Related Antibodies

Top Publications Citing Use of Products

104 Publications Citing Use of MCE Telaglenastat hydrochloride

WB
Cell Proliferation/Viability Assay
Cell Imaging/Staining

    Telaglenastat hydrochloride purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2024 Jan 24:S0016-5085(24)00064-7.  [Abstract]

    Phase-contrast images of dysplastic organoids treated with dimethyl sulfoxide (DMSO; vehicle), GSK2837808A (LDH inhibitor; 10 μmol/L), 6-aminonicotinamide (6-AN, glucose-6-phosphate dehydrogenase [G6PD] inhibitor; 50 μmol/L), telaglenastat (GLS1 inhibitor; 1 μmol/L) for 3 days.

    Telaglenastat hydrochloride purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2024 Jan 24:S0016-5085(24)00064-7.  [Abstract]

    Phase-contrast images of dysplastic organoids treated with dimethyl sulfoxide (DMSO; vehicle), GSK2837808A (LDH inhibitor; 10 μM), 6-aminonicotinamide (G6PD inhibitor; 50 μM), telaglenastat (GLS1 inhibitor; 1 μM) for 3 days.

    Telaglenastat hydrochloride purchased from MedChemExpress. Usage Cited in: Pathol Int. 2023 May;73(5):181-187.  [Abstract]

    Telaglenastat (1, 2.5, 5, 10 μM; 5 days) inhibits the proliferation of DeGISTL1 cells dose-dependently.

    Telaglenastat hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Jun;40(6):814-822.  [Abstract]

    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.

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

    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 MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Oct 2;504(2):415-421.  [Abstract]

    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 MedChemExpress. Usage Cited in: Blood Adv. 2017 Jul 14;1(17):1296-1305.  [Abstract]

    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.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    Telaglenastat hydrochloride Related Antibodies

    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].

    MedChemExpress (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.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    [H]Cl.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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (164.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6446 mL 8.2231 mL 16.4463 mL
    5 mM 0.3289 mL 1.6446 mL 3.2893 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Working solution concentration: mg/mL
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6446 mL 8.2231 mL 16.4463 mL 41.1157 mL
    5 mM 0.3289 mL 1.6446 mL 3.2893 mL 8.2231 mL
    10 mM 0.1645 mL 0.8223 mL 1.6446 mL 4.1116 mL
    15 mM 0.1096 mL 0.5482 mL 1.0964 mL 2.7410 mL
    20 mM 0.0822 mL 0.4112 mL 0.8223 mL 2.0558 mL
    25 mM 0.0658 mL 0.3289 mL 0.6579 mL 1.6446 mL
    30 mM 0.0548 mL 0.2741 mL 0.5482 mL 1.3705 mL
    40 mM 0.0411 mL 0.2056 mL 0.4112 mL 1.0279 mL
    50 mM 0.0329 mL 0.1645 mL 0.3289 mL 0.8223 mL
    60 mM 0.0274 mL 0.1371 mL 0.2741 mL 0.6853 mL
    80 mM 0.0206 mL 0.1028 mL 0.2056 mL 0.5139 mL
    100 mM 0.0164 mL 0.0822 mL 0.1645 mL 0.4112 mL
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    Telaglenastat hydrochloride Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Telaglenastat1874231-60-3CB-839CB839CB 839GlutaminaseAutophagyselectivetriple-negativebreastcancerTNBCantiproliferativeHCC-1806PDACcellsplicevariantsInhibitorinhibitorinhibit

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