Telaglenastat

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].

Product Specifications

CAS Number

[1439399-58-2]

Product Name Alternative

CB-839

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Glutaminase

Type

Reference compound

Related Pathways

Autophagy; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CB-839.html

Purity

99.92

Solubility

DMSO : 35 mg/mL (ultrasonic)

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

Molecular Formula

C26H24F3N7O3S

Molecular Weight

571.57

Precautions

H302, H315, H319, H335

References & Citations

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