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GNE-617

Catalog No.GC16041

GNE-617 Chemical Structure

NAMPT inhibitor

Size Price Stock Qty
10mM (in 1mL DMSO)
$248.00
In stock
2mg
$94.00
In stock
5mg
$149.00
In stock
10mg
$224.00
In stock
50mg
$597.00
In stock
100mg
$804.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

hARPE-19 and hRPEpC cell lines

Preparation method

The solubility of this compound in DMSO is > 21.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.0032, 0.016, 0.08, 0.4, 2, and 10 µM, 3 d

Applications

In rat retinal mixed cell population, cytotoxicity induced by GNE-617 is correlated with activity and potency. And human cells were more sensitive to cytotoxicity induced by GNE-617 than rat cells.

Animal experiment [2]:

Animal models

Female BALB/c SCID mice

Dosage form

Oral administration, 5-30 mg/kg, twice daily for 5 days

Application

When treated with GNE-617, a significant time-dependent decrease in NAD levels was observed in PC3 and HT-1080 xenograft tumors. In the HT-1080 xenograft model, GNE-617 decreased tumor NAD levels in a dose-dependent manner.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Zabka T S, Singh J T, Dhawan P, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase[J]. Toxicological Sciences, 2014: kfu268.

[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[J]. Neoplasia, 2013, 15(12): 1314IN1-1329IN3.

Background

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

GNE-617 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 shows the most optimal combination of in vitro metabolic stability, MDCK permeability and protein binding. Besides that, GNE-617 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 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

Cas No. 1362154-70-8 SDF
Chemical Name N-(4-((3,5-difluorophenyl)sulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carboxamide
Canonical SMILES FC1=CC(S(C2=CC=C(C=C2)CNC(C(C=C3)=CN4C3=NC=C4)=O)(=O)=O)=CC(F)=C1
Formula C21H15F2N3O3S M.Wt 427.42
Solubility ≥ 21.35mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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