GNE-618

Name: GNE-618
Brand: TargetMol
SKU: T15403
Rating: 4.5 (1 reviews)

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Catalog No. T15403Cas No. 1362151-42-5

GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.

GNE-618

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Catalog No. T15403Cas No. 1362151-42-5

GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$178	8-10 weeks	8-10 weeks
25 mg	$637	8-10 weeks	8-10 weeks
50 mg	$828	8-10 weeks	8-10 weeks
100 mg	$1,240	8-10 weeks	8-10 weeks
1 mL x 10 mM (in DMSO)	$183	8-10 weeks	8-10 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-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.
Targets&IC50	NAMPT:6 nM
In vitro	GNE-618 decreases levels of NAD (EC50: 2.6 nM in the NSCLC cell line Calu-6). GNE-618 also reduces cellular proliferation of Calu-6 cells as determined using two different assay formats, either measuring ATP (EC50: 13.6 nM) or total protein content (SRB assay; EC50: 25.8 nM). GNE-618 (10-30 nM; 72 hours) displays an increase in the sub-2N population and a reduction in the percentage of cells in the G1 and M phases of the cell cycle in Calu-6 cells.
In vivo	In the STO#81 patient-derived gastric cancer model, GNE-618 administered orally at a dosage of 100 mg/kg twice daily for 5 days significantly inhibits tumor growth by 88%, while having minimal effects on body weight.

Chemical Properties

Molecular Weight	460.43
Formula	C₂₁H₁₅F₃N₄O₃S
Cas No.	1362151-42-5
Smiles	FC(F)(F)c1cccc(c1)S(=O)(=O)c1ccc(CNC(=O)c2cnc3[nH]ncc3c2)cc1
Relative Density.	1.479 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc