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GNE-617 hydrochloride

Catalog No.
B1309
NAMPT inhibitor, potent and competitive
Grouped product items
SizePriceStock Qty
2mg
$221.00
In stock
5mg
$331.00
In stock
10mg
$520.00
Ship with 10-15 days
50mg
$1,319.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

GNE-617 hydrochloride is a potent and competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with IC50 value of 5nM [1].

GNE-617 hydrochloride is a potent inhibitor of NAMPT. It reduces the NAD levels in a > 95% reduction in both NAPRT1-deficient and NAPRT1-proficient cell lines and exerts EC50 values ranging from 0.54nM to 4.69nM. In the invitro 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. Moreover, 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].

References:
[1] Zheng X, Bauer P, Baumeister T, et al.  Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors. Journal of medicinal chemistry, 2013, 56(16): 6413-6433.
[2] O'Brien T, Oeh J, Xiao Y, et al.  Supplementation of Nicotinic Acid with NAMPT Inhibitors Results in Loss of In Vivo Efficacy in NAPRT1-Deficient Tumor Models. Neoplasia, 2013, 15(12): 1314-IN3.

Chemical Properties

StorageStore at -20°C
M.Wt463.88
FormulaC21H16ClF2N3O3S
SolubilitySoluble in DMSO
Chemical Name(Z)-N-(4-((3,5-difluorophenyl)sulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carbimidic acid hydrochloride
SDFDownload SDF
Canonical SMILESFC1=CC(F)=CC(S(C2=CC=C(C/N=C(O)/C3=CN4C=CN=C4C=C3)C=C2)(=O)=O)=C1.Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

GNE-617 hydrochloride