Telaglenastat (Synonyms: CB-839)

Name: Telaglenastat
Brand: MedChemExpress
SKU: HY-12248
Rating: 5.0 (104 reviews)

Cat. No.: HY-12248 Purity: 99.82%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

CAS No. : 1439399-58-2

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	Get quote
5 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 104 publication(s) in Google Scholar

Other Forms of Telaglenastat:

Telaglenastat hydrochloride In-stock
Telaglenastat (Standard) Get quote

104 Publications Citing Use of MCE Telaglenastat

Cell Proliferation/Viability Assay

Cell Imaging/Staining

: Telaglenastat 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 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 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 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: 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

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 3 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 3 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	0.026 3 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 3 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	0.04 3 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	0.04 3 Compound: CB839	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 5 days by EZMTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 5 days by EZMTT assay	[PMID: 37465295]
A549	IC₅₀	0.04 3 Compound: CB839	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 5 days by EZMTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 5 days by EZMTT assay	[PMID: 37465295]
A549	IC₅₀	0.026 3 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	6 1 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]
A549	IC₅₀	18.78 1 Compound: 4; CB-839	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-glo assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-glo assay	[PMID: 37849538]
CAKI-1	IC₅₀	0.04 3 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]
CAKI-1	IC₅₀	0.04 3 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 3 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]
CT26	IC₅₀	0.42 3 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]
A549	IC₅₀	6 1 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]
H22	IC₅₀	>10 3 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	> 10 3 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	>10 3 Compound: CB839	Antiproliferative activity against mouse H22 cells assessed as cell growth inhibition incubated for 5 days by EZMTT assay Antiproliferative activity against mouse H22 cells assessed as cell growth inhibition incubated for 5 days by EZMTT assay	[PMID: 37465295]
H22	IC₅₀	1.34 3 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 1 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]
CAKI-1	IC₅₀	0.04 3 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]
H22	IC₅₀	1.34 3 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]
A549	IC₅₀	6 1 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]
HCC827	IC₅₀	51.42 3 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]
CT26	IC₅₀	0.42 3 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]
HCC827	IC₅₀	51.42 3 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 3 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 3 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	0.028 3 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 3 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]
H22	IC₅₀	1.34 3 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]
HCT-116	IC₅₀	0.06 3 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]
H22	IC₅₀	> 10 3 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]
HCT-116	IC₅₀	0.11 3 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]
HCT-116	IC₅₀	0.11 3 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]
H22	IC₅₀	> 10 3 Compound: CB839	Antiproliferative activity against mouse H22 cells assessed as cell growth inhibition incubated for 5 days by EZMTT assay Antiproliferative activity against mouse H22 cells assessed as cell growth inhibition incubated for 5 days by EZMTT assay	[PMID: 37465295]
HT-1080	IC₅₀	44.38 3 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]
HCT-116	IC₅₀	0.56 3 Compound: CB839	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay	[PMID: 36525694]
HCT-116	IC₅₀	0.06 3 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]
MDA-MB-231	IC₅₀	33 1 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]
HCC1806	IC₅₀	100 1 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]
MDA-MB-231	IC₅₀	50 1 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]
A549	IC₅₀	18.78 1 Compound: 4; CB-839	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-glo assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-glo assay	[PMID: 37849538]
HCC827	IC₅₀	51.42 3 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]
HT-1080	IC₅₀	44.38 3 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-436	IC₅₀	0.41 3 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 3 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-231	IC₅₀	33 1 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 1 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	0.52 3 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]
MDA-MB-436	IC₅₀	0.43 3 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]
NCI-H1703	GI₅₀	0.008 3 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 3 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]
MDA-MB-436	IC₅₀	0.52 3 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]
HCT-116	IC₅₀	0.028 3 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]
NCI-H460	IC₅₀	0.036 3 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]
HCT-116	IC₅₀	0.06 3 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]
MDA-MB-436	IC₅₀	0.41 3 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]
HCT-116	IC₅₀	0.06 3 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]
HCC1806	IC₅₀	100 1 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]
NCI-H1703	GI₅₀	0.008 3 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]
HCT-116	IC₅₀	0.11 3 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]
HCT-116	IC₅₀	0.56 3 Compound: CB839	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay	[PMID: 36525694]
NCI-H358	IC₅₀	>1 3 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 3 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]
SW1990	IC₅₀	13.06 3 Compound: 16; CB-839	Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay	[PMID: 36996714]
HT-1080	IC₅₀	44.38 3 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 1 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 1 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 3 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 3 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 3 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 3 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 3 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 3 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]
SW1990	IC₅₀	13.06 3 Compound: 16; CB-839	Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay	[PMID: 36996714]

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

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 : 35 mg/mL (61.23 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
10 mM	0.1750 mL	0.8748 mL	1.7496 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 5 mg/mL (8.75 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
Protocol 3

Add each solvent one by one: 20% SBE-β-CD/10 mM Trisodium citrate adjusted to pH 2.0 with HCl
Solubility: 5 mg/mL (8.75 mM); Clear solution; Need ultrasonic and adjust pH to 2 with 1M HCl and heat to 55°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (275 KB) 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

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

Telaglenastat 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.

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Product Name			Requested Quantity *
Applicant Name *			Salutation
Email Address *			Phone Number *
Department			Organization Name *
City			State
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Telaglenastat (Synonyms: CB-839)

Customer Review

Other Forms of Telaglenastat:

104 Publications Citing Use of MCE Telaglenastat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Telaglenastat Related Classifications

Keywords:

Your Recently Viewed Products:

Name
Email *

	Sorry, but the email address you supplied was invalid.

Telaglenastat (Synonyms: CB-839)

Customer Review

Other Forms of Telaglenastat:

Telaglenastat Related Antibodies

104 Publications Citing Use of MCE Telaglenastat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Telaglenastat Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Telaglenastat Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report