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Telaglenastat

CAT: 0804-HY-12248-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12248-01Size:5 mg
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2

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