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GNE-617

Catalog No. T4335 CAS 1362154-70-8

Synonyms: GNE617, GNE 617

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

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GNE-617, CAS 1362154-70-8

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Purity: 98%

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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 rats, GNE-617 hydrochloride (administered QD) and GNE-875 (administered BID) are associated with more severe retinal toxicity at similar exposures and dosing duration compared with GMX-1778 (administered BID). The mouse efficacy studies using GNE-617, GNE-618, and GMX-1778 are designed to assess efficacy and opportunistically used to assess retinal toxicity in mice. NAMPTi retinal toxicity is observed with GNE-617 and GMX-1778; nevertheless, the different study durations between GNE-617 and GMX-1778 do not allow for direct comparison of retinal toxicity.
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) .

Synonyms	GNE617, GNE 617
Molecular Weight	427.43
Formula	C21H15F2N3O3S
CAS No.	1362154-70-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 42.85 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Shames DS, et al. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors. Clin Cancer Res. 2013 Dec 15;19(24):6912-23. 2. Zabka TS, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Fluorochemical Library Anti-Cancer Active Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library

Related Products

Related compounds with same targets

Nampt activator-1 STF-118804 Nampt-IN-1 KPT9274 GNE-617 (E)-Daporinad CHS-828 GNE-618

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Keywords

GNE-617 1362154-70-8 代谢 NAMPT Pre-B cell colony enhancing factor Inhibitor GNE 617 GNE617 PBEF Visfatin Nicotinamide phosphoribosyl transferase inhibit inhibitor

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