Telaglenastat (CB-839) - Moligand™, 10mM in DMSO , Glutaminase kidney isoform, mitochondrial inhibitor, CAS No.1439399-58-2, Glutaminase kidney isoform, mitochondrial inhibitor

CAS: 1439399-58-2 Cat. No.: T408493 Peso molecular: 571.57

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-2-pyridineacetamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Telaglenastat (CB-839) Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.
In vitro

CB-839 exhibits time-dependent and slowly reversible kinetics. IC50 values for glutaminase inhibition by CB-839 following preincubation with rHu-GAC for-1 hour are < 50 nmol/L, at least 13-fold lower than with BPTES. CB-839 has antiproliferative activity in a triple-negative breast cancer (TNBC) cell line, HCC-1806, while no antiproliferative activity is observed in an estrogen receptor–positive cell line, T47D.

In vivo

In the mouse TNBC model, single agent CB-839 (200 mg/kg, p.o.) suppresses tumor growth by 61% relative to vehicle control. In the mouse JIMT-1 xenograft model, CB-839 alone (200 mg/kg, p.o.) results in 54% tumor growth inhibition (TGI) relative to vehicle control, combination of CB-839 (200 mg/kg, p.o.) with paclitaxel (10 mg/kg, p.o.) largely suppresses the regrowth of the tumors resulting in a TGI relative to vehicle control of 100%.
Cell Data

cell lines：SKGT-4 and JHESO cells

Concentrations：0.1-1000 nM

Incubation Time：72 h

Powder Purity:≥98%

Specifications

Sinónimos

N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1, 3, 4-thiadiazol-2-yl]-2-pyridineacetamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Glutaminase kidney isoform, mitochondrial inhibitor

Propiedades del producto

• ALogP: 3.6

Nombres e identificadores

• Isómeros SMILES: C1=CC=NC(=C1)CC(=O)NC2=NN=C(S2)CCCCC3=NN=C(C=C3)NC(=O)CC4=CC(=CC=C4)OC(F)(F)F
• Peso molecular: 571.57
• Reaxy-Rn: 23710292
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23710292&ln=

Objetivos asociados (humanos)

GLS Tchem Glutaminase kidney isoform, mitochondrial (17 Activities)

Discover Target: GLS

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Punto de fusión (°C): 186- 189° C

Referencias

1. Benjian Gao, Dongning Zheng, Hong Liu, Yu Guo, Yuntao Ye, Zhou Chen, Fengyi Yang, Jie Liu, Guangnian Zhang, Guoying Feng, Yongfa Liu, Qiang Wang, Song Su, Xiaoli Yang, Bo Li.  (2025)  Asparagine synthetase modulates glutaminase inhibitor sensitivity through metabolic reprogramming and serves as a prognostic biomarker in hepatocellular carcinoma.  Redox Biology,      [PMID:40779838] [10.1016/j.redox.2025.103813]

2. Haofan Hu, Shangwu Ning, Furong Liu, Ze Zhang, Weifeng Zeng, Yachong Liu, Zhibin Liao, Hongwei Zhang, Zhanguo Zhang.  (2025)  Hafnium Metal–Organic Framework-Based Glutamine Metabolism Disruptor For Potentiating Radio-Immunotherapy in MYC-Amplified Hepatocellular Carcinoma.  ACS Applied Materials & Interfaces,      [PMID:40116395] [10.1021/acsami.4c21998]

3. Zhen Li, Fang Li, Wang Song, Chun-mei Long, Xin Zeng, Wen-kai Guo, Bin Chen, Tai-xin Jia, Li Lu.  (2026)  Ampelopsin preserves glutamate homeostasis against cerebral ischemia.  BIOMEDICINE & PHARMACOTHERAPY,      [PMID:41529512] [10.1016/j.biopha.2026.119002]

4. Ruo-Yun Zhang, Wei Yue, Yang Xuan, Long Qi, Lin-Lin Guo, Zhen-Zhen Zhu, Ming Yang, Zhang-Jie Pu, Guo-Qiang Li, Xin-Yi Mao, Ding Zhou, Zhao-Wei Zhang.  (2026)  Injectable anti-inflammatory nanofiber hydrogel reprograms immunosuppressive tumor microenvironment via cascade-amplified immunogenic cell death.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2026.173232]