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GNE-617

GNE-617
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Purity:99.97%
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GNE-617

Catalog No. T4335Cas No. 1362154-70-8
GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of cancer.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePrice/USDAvailabilityQuantity
1 mg$34In Stock
2 mg$48In Stock
5 mg$77In Stock
10 mg$126In Stock
25 mg$230In Stock
50 mg$369In Stock
100 mg$549In Stock
500 mg$1,190In Stock
1 mL x 10 mM (in DMSO)$78In Stock
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Product Introduction

Bioactivity
Description
GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of cancer.
In vitro
In A549 cell, GNE-617 inhibits NAMPT (IC50=18.9 nM) .
In vivo
In rat studies, GNE-617 hydrochloride (QD) and GNE-875 (BID) demonstrated greater retinal toxicity at comparable exposures and durations of dosing than did GMX-1778 (BID). The efficacy studies in mice, which evaluated GNE-617, GNE-618, and GMX-1778, also opportunistically investigated retinal toxicity. NAMPTi-induced retinal toxicity was identified in cases involving GNE-617 and GMX-1778. However, varying study durations for GNE-617 and GMX-1778 preclude a direct comparison of their retinal toxicity profiles.
Kinase Assay
For RNA interference (RNAi), A549 cells are plated at 1,500 cells per well in 96-well plates, allowed to adhere for 24 hours, and transfected with 25 nM siRNA oligonucleotide using Dharmafect 4. Transfected cells are treated with the indicated concentrations of GNE-617 (0.1, 1 , 10 , 100 , and 1000 nM) for 72 hours and viability is evaluated with CellTiter-Glo. Lysates for detection of NAPRT1 protein are collected 72 hours after transfection of 1 million A549 cells in 10 cm dishes. For NAPRT1 re-expression, RERF-LC-MS cells are transfected with pCMV6-AC.NAPRT1 and empty vector pCMV6-AC using Amaxa Nucleofector technology and selected with Geneticin
Cell Research
GNE-617 is dissolved in DMSO and stored, and then diluted with appropriate media before use.Cells are grown in RPMI-1640 medium supplemented with 10% FBS and 2 mM glutamine and passaged not more than 20 times after thawing. To determine the IC50 values and nicotinic acid rescue status, cells are treated with nine point dose titrations of GNE-617 with or without 10 μM nicotinic acid. At 96 hours post-drug addition, the GNE-617-treated cells are evaluated using CyQUANT Direct Cell Proliferation Assay followed by CellTiter-Glo Luminescent Cell Viability Assay quantified with a Wallac EnVision 2104 Multilabel Reader. IC50 values are calculated using XLfit 5.1. To examine the protein level, cells are lysed in ice-cold radioimmunoprecipitation assay buffer, run on SDS-PAGE (4%-12% Bis-Tris), and evaluated by Western blotting using antibodies directed against NAPRT1 and β-actin
Animal Research
Male na?ve Sprague Dawley rats are administered once daily via oral gavage with GNE-617( 30?mg/kg), formulated as a solution in the vehicle of 60% polyethylene glycol (PEG 400)/10% ethanol/30% 5% dextrose in water (D5W) .
AliasGNE617
Chemical Properties
Molecular Weight427.42
FormulaC21H15F2N3O3S
Cas No.1362154-70-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 25 mg/mL (58.49 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3396 mL11.6981 mL23.3962 mL116.9810 mL
5 mM0.4679 mL2.3396 mL4.6792 mL23.3962 mL
10 mM0.2340 mL1.1698 mL2.3396 mL11.6981 mL
20 mM0.1170 mL0.5849 mL1.1698 mL5.8490 mL
50 mM0.0468 mL0.2340 mL0.4679 mL2.3396 mL

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