Name: Telaglenastat hydrochloride
Rating: 5 (10 reviews)

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HIT ID:HIT214322857
Cas No:1874231-60-3
常用名:Telaglenastat hydrochloride
别名:CB-839 hydrochloride
IUPAC:N-[6-(4-{5-[2-(pyridin-2-yl)acetamido]-1,3,4-thiadiazol-2-yl}butyl)pyridazin-3-yl]-2-[3-(trifluoromethoxy)phenyl]acetamide hydrochloride
IUPAC:N-[6-(4-{5-[2-(pyridin-2-yl)acetamido]-1,3,4-thiadiazol-2-yl}butyl)pyridazin-3-yl]-2-[3-(trifluoromethoxy)phenyl]acetamide hydrochloride
InChI key:NMVMURBPQFKTAX-UHFFFAOYSA-N

分子式:C26H25ClF3N7O3S
分子量:608.04
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:Cl.FC(F)(F)Oc1cccc(CC(=O)Nc2ccc(CCCCc3nnc(NC(=O)Cc4ccccn4)s3)nn2)c1
SMILES:Cl.FC(F)(F)Oc1cccc(CC(=O)Nc2ccc(CCCCc3nnc(NC(=O)Cc4ccccn4)s3)nn2)c1

Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1). It selectively inhibits the splice variants of GLS1, specifically KGA (kidney-type glutaminase) and GAC (glutaminase C), as compared to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain. In addition, it induces autophagy and exhibits antitumor activity.

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