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

Catalog No. T22801

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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Pack Size	Price	Availability
2 mg	$160	Backorder
5 mg	$237	Backorder
10 mg	$371	Backorder
50 mg	$938	Backorder

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Product Introduction

Bioactivity

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
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].
Alias	GNE-617 hydrochloride

Chemical Properties

Molecular Weight	463.88
Formula	C21H16ClF2N3O3S
Cas No.

Storage & Solubility Information

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
Solubility Information	DMSO: Soluble

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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