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

Catalog No. T22801   CAS T22801
Synonyms: GNE-617 hydrochloride

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).

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GNE-617 hydrochloride (1362154-70-8 free base) Chemical Structure
GNE-617 hydrochloride (1362154-70-8 free base), CAS T22801
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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 vitro 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.
In vivo 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].
Synonyms GNE-617 hydrochloride
Molecular Weight 463.88
Formula C21H16ClF2N3O3S
CAS No. T22801

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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DMSO: Soluble

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Keywords

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