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Telaglenastat [1439399-58-2]

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Cat# HY-12248-5mg

Size : 5mg

Brand : MedChemExpress

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Télaglenastat (CB-839) est un inhibiteur de la glutaminase 1 (GLS1) sélectif, réversible et oralement premier de sa catégorie. Télaglenastat inhibe sélectivement les variantes d'épissage GLS1 KGA (glutaminase de type rénal) et GAC (glutaminase C) par rapport à GLS2. Les IC50 sont respectivement de 23 nM et 28 nM pour la glutaminase endogène dans les reins et le cerveau de souris. Telaglenastat déclenche l'autophagie et a une activité antitumorale.

Telaglenastat (CB-839) ist ein erstklassiger, selektiver, reversibler und oral wirksamer glutaminase 1 (GLS1)-Inhibitor. Telaglenastat hemmt selektiv die GLS1-Spleissvarianten KGA (KGA (kidney-type glutaminase)) und (GAC (glutaminase C)) im Vergleich zu GLS2. Die IC50s betragen 23 nM und 28 nM für die endogene glutaminase in der Niere bzw. im Gehirn der Maus. Telaglenastat inudiert die autophagy und besitzt Antitumor-Aktivität.

Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat 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 inuduces autophagy and has antitumor activity.

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

Telaglenastat Chemical Structure

Telaglenastat Chemical Structure

CAS No. : 1439399-58-2

This product is a controlled substance and not for sale in your territory.

Based on 77 publication(s) in Google Scholar

Other Forms of Telaglenastat:

  • Telaglenastat hydrochloride Get quote

    Telaglenastat purchased from MedChemExpress. Usage Cited in: Pathol Int. 2023 Feb 24.  [Abstract]

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

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

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

    Telaglenastat 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.
    Description

    Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat 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 inuduces autophagy and has antitumor activity[1].

    IC50 & Target

    IC50: 23 nM (GLS1 in kidney), 28 nM (GLS1 in brain), >1 μM (GLS2 in liver)[1]
    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    0.026 μM
    Compound: CB-839
    Antiproliferative activity against human A549 cells incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human A549 cells incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 36038117]
    A549 IC50
    0.04 μM
    Compound: CB-839
    Antiproliferative activity against human A549 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against human A549 cells after 5 days by EZMTT reagent-based assay
    		[PMID: 30543285]
    A549 IC50
    6 nM
    Compound: 4, CB-839
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-fluor assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-fluor assay
    		[PMID: 33118821]
    CAKI-1 IC50
    0.04 μM
    Compound: CB-839
    Antiproliferative activity against human Caki1 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against human Caki1 cells after 5 days by EZMTT reagent-based assay
    		[PMID: 30543285]
    CT26 IC50
    0.42 μM
    Compound: I-6; CB839
    Antiproliferative activity against mouse CT26 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against mouse CT26 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 35428013]
    H22 IC50
    > 10 μM
    Compound: CB-839
    Antiproliferative activity against mouse H22 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against mouse H22 cells after 5 days by EZMTT reagent-based assay
    		[PMID: 30543285]
    H22 IC50
    1.34 μM
    Compound: I-6; CB839
    Antiproliferative activity against mouse H22 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against mouse H22 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 35428013]
    HCC1806 IC50
    100 nM
    Compound: 71; CB-839
    Anticancer activity against human HCC1806 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Blue assay
    Anticancer activity against human HCC1806 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Blue assay
    		[PMID: 33650861]
    HCC827 IC50
    51.42 μM
    Compound: CB-839
    Cytotoxicity against human erlotinib-resistant HCC827 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    Cytotoxicity against human erlotinib-resistant HCC827 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    		[PMID: 28174105]
    HCT-116 IC50
    0.028 μM
    Compound: CB-839
    Antiproliferative activity against human HCT116 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against human HCT116 cells after 5 days by EZMTT reagent-based assay
    		[PMID: 30543285]
    HCT-116 IC50
    0.06 μM
    Compound: I-6; CB839
    Antiproliferative activity against human HCT-116 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 35428013]
    HCT-116 IC50
    0.06 μM
    Compound: CB839
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 31603674]
    HCT-116 IC50
    0.11 μM
    Compound: CB839; I-4
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 33792311]
    HT-1080 IC50
    44.38 μM
    Compound: CB-839
    Cytotoxicity against human HT1080 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    Cytotoxicity against human HT1080 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    		[PMID: 28174105]
    MDA-MB-231 IC50
    33 nM
    Compound: CB-839
    Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry
    Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry
    		[PMID: 26988803]
    MDA-MB-231 IC50
    50 nM
    Compound: 71; CB-839
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Blue assay
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Blue assay
    		[PMID: 33650861]
    MDA-MB-436 IC50
    0.41 μM
    Compound: I-6; CB839
    Antiproliferative activity against human MDA-MB-436 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-436 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 35428013]
    MDA-MB-436 IC50
    0.43 μM
    Compound: CB839; I-4
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 33792311]
    MDA-MB-436 IC50
    0.52 μM
    Compound: CB839
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 31603674]
    NCI-H1703 GI50
    0.008 μM
    Compound: 5; CB-839
    Antiproliferative activity against human NCI-H1703 cells assessed as reduction in cell growth after 5 days by SYTOX green staining-based assay
    Antiproliferative activity against human NCI-H1703 cells assessed as reduction in cell growth after 5 days by SYTOX green staining-based assay
    		[PMID: 31199640]
    NCI-H358 IC50
    > 1 μM
    Compound: CB-839
    Antiproliferative activity against human NCI-H358 cells incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human NCI-H358 cells incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 36038117]
    NCI-H460 IC50
    0.036 μM
    Compound: CB-839
    Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 36038117]
    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 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.
    Clinical Trial
    Molecular Weight

    571.57

    Formula

    C26H24F3N7O3S
    CAS No.

    1439399-58-2
    Appearance

    Solid

    Color

    Off-white to yellow

    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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (87.48 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 1.7496 mL 8.7478 mL 17.4957 mL
    5 mM 0.3499 mL 1.7496 mL 3.4991 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: 10 mg/mL (17.50 mM); Clear solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  70% PEG300    30% (20% SBE-β-CD in Saline)

      Solubility: 4 mg/mL (7.00 mM); Suspended solution; Need ultrasonic and warming and heat to 55°C

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.82%

    SDS (393 KB)

    COA (244 KB) HNMR (240 KB) LCMS (122 KB) Elemental Analysis Report (102 KB)

    Handling Instructions (2659 KB)
    References

    • [1]. Gross MI, et al. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901.  [Content Brief]

      [2]. Biancur DE, et al. Compensatory metabolic networks in pancreatic cancers upon perturbation of glutaminemetabolism. Nat Commun. 2017 Jul 3;8:15965.  [Content Brief]

      [3]. Zhou WJ, et al. Estrogen inhibits autophagy and promotes growth of endometrial cancer by promoting glutamine metabolism. Cell Commun Signal. 2019 Aug 20;17(1):99.  [Content Brief]

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7496 mL 8.7478 mL 17.4957 mL 43.7392 mL
    5 mM 0.3499 mL 1.7496 mL 3.4991 mL 8.7478 mL
    10 mM 0.1750 mL 0.8748 mL 1.7496 mL 4.3739 mL
    15 mM 0.1166 mL 0.5832 mL 1.1664 mL 2.9159 mL
    20 mM 0.0875 mL 0.4374 mL 0.8748 mL 2.1870 mL
    25 mM 0.0700 mL 0.3499 mL 0.6998 mL 1.7496 mL
    30 mM 0.0583 mL 0.2916 mL 0.5832 mL 1.4580 mL
    40 mM 0.0437 mL 0.2187 mL 0.4374 mL 1.0935 mL
    50 mM 0.0350 mL 0.1750 mL 0.3499 mL 0.8748 mL
    60 mM 0.0292 mL 0.1458 mL 0.2916 mL 0.7290 mL
    80 mM 0.0219 mL 0.1093 mL 0.2187 mL 0.5467 mL
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    Telaglenastat Related Classifications

    Help & FAQs

    Keywords:

    Telaglenastat1439399-58-2CB-839CB839CB 839GlutaminaseAutophagyselectivetriple-negativebreastcancerTNBCantiproliferativeHCC-1806PDACcellsplicevariantsInhibitorinhibitorinhibit

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