| Identification | Back Directory | [Name]
2-Pyridineacetamide, N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-, hydrochloride (1:1) | [CAS]
1874231-60-3 | [Synonyms]
CB-839 hydrochloride
Telaglenastat hydrochloride
2-Pyridineacetamide, N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-, hydrochloride (1:1) | [Molecular Formula]
C26H25ClF3N7O3S | [MOL File]
1874231-60-3.mol | [Molecular Weight]
608.04 |
| Hazard Information | Back Directory | [Uses]
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride 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 hydrochloride inudces autophagy and has antitumor activity[1]. | [in vivo]
Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1]. | 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.
|
| [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. DOI:10.1158/1535-7163.MCT-13-0870
[2] Biancur DE, et al. Compensatory metabolic networks in pancreatic cancers upon perturbation of glutaminemetabolism. Nat Commun. 2017 Jul 3;8:15965. DOI:10.1038/ncomms15965
[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. DOI:10.1186/s12964-019-0412-9 |
|
|