Reagents and instruments for immunology, cell biology and molecular biology.

Telaglenastat [1439399-58-2]

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Cat# HY-12248-10mg

Size : 10mg

Brand : MedChemExpress

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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.

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.

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%

Data Sheet (275 KB) SDS (393 KB)

COA (244 KB) HNMR (239 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]

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Cat# HY-12248-10mg

Brand : MedChemExpress

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