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GNE-617

Catalog No. T4335Cas No. 1362154-70-8
Alias GNE617

GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of cancer.

GNE-617

GNE-617

Purity: 99.97%
Catalog No. T4335Alias GNE617Cas No. 1362154-70-8
GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of cancer.
Pack SizePriceAvailabilityQuantity
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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Purity:99.97%
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Product Introduction

Bioactivity
Description
GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of cancer.
Targets&IC50
NAMPT:5 nM
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 | Shipping with blue ice.
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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