Telaglenastat hydrochloride (Synonyms: CB-839 hydrochloride)

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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.

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Telaglenastat hydrochloride Chemical Structure

CAS No. : 1874231-60-3

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57 Publications Citing Use of MCE Telaglenastat hydrochloride

Proliferation Assay

: Telaglenastat hydrochloride 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 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: Cancer Discov. 2017 Apr;7(4):380-390. [Abstract]; MEFs treated with 12.5 nM CB-839 or control (one-way ANOVA).

: 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.

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Description

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.

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

608.04

Formula

C₂₆H₂₅ClF₃N₇O₃S

CAS No.

1874231-60-3

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

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

Purity & Documentation

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]

Telaglenastat hydrochloride Related Classifications

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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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