GNE-617 hydrochloride is a potent and competitive inhibitor of nicotinamide phosphoribosyltransferase (IC50: 5nM). GNE-617 hydrochloride reduces the NAD levels in a >95% reduction in both NAPRT1-deficient and NAPRT1-proficient cell lines and exerts (EC50: 0.54nM to 4.69nM).

In the in-vitro ADME assessments, GNE-617 hydrochloride shows the most optimal combination of in vitro metabolic stability, MDCK permeability, and protein binding. Besides that, GNE-617 hydrochloride has potent antiproliferation effects on various cell lines. The IC50 values of it in U251, HT1080, PC3, MiaPaCa2 and HCT116 cell lines are 1.8nM, 2.1nM, 2.7nM, 7.4nM and 2nM, respectively.

GNE-617 hydrochloride also shows significant antitumor effects on U251 human glioblastoma tumor xenografts in mice and has no obvious effect on body weight loss [1][2].

T22801

C21H16ClF2N3O3S

463.88

GNE-617 hydrochloride;GNE-617 hydrochloride (1362154-70-8 free base)

DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years