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

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Catalog No. T22801
Alias 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).

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

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

Copy Product Info
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Catalog No. T22801Alias 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).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$1606-8 weeks6-8 weeks
5 mg$2376-8 weeks6-8 weeks
10 mg$3716-8 weeks6-8 weeks
50 mg$9386-8 weeks6-8 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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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: 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].
SynonymsGNE-617 hydrochloride
Chemical Properties
Molecular Weight463.88
FormulaC21H16ClF2N3O3S
SmilesFC1=CC(F)=CC(S(C2=CC=C(C/N=C(O)/C3=CN4C=CN=C4C=C3)C=C2)(=O)=O)=C1.Cl
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: Soluble

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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