Art. -Nr.: HY-15766

GNE-617

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC₅₀ of 5 nM and exhibits efficacy in xenograft models of cancer.

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Reinheit: 99.58%
CAS. Nr.: 1362154-70-8
Formel: C₂₁H₁₅F₂N₃O₃S
Molecular Weight:427.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GNE-617 Chemical Structure

CAS. Nr.: 1362154-70-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC₅₀ of 5 nM and exhibits efficacy in xenograft models of cancer.

IC₅₀ & Target

IC50: 5 nM (NAMPT)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.002 μM Compound: 1; GNE-617	Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay	[PMID: 27541271]
A2780	IC₅₀	0.002 μM Compound: 58	Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis	[PMID: 23859118]
B16-F10	IC₅₀	71 nM Compound: 4	Antiproliferative activity against mouse B16F10 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against mouse B16F10 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
Calu-6	IC₅₀	5 nM Compound: 4	Antiproliferative activity against human Calu6 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human Calu6 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
COS-1	IC₅₀	5 nM Compound: 4	Cytotoxicity against African green monkey COS1 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Cytotoxicity against African green monkey COS1 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
COS-7	IC₅₀	9 nM Compound: 4	Cytotoxicity against African green monkey COS7 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Cytotoxicity against African green monkey COS7 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
HCT-116	IC₅₀	2 nM Compound: 4	Antiproliferative activity against human HCT116 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human HCT116 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
HCT-116	IC₅₀	2 nM Compound: 58	Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs	[PMID: 23859118]
HT-1080	IC₅₀	2 nM Compound: 4	Antiproliferative activity against human HT1080 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human HT1080 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
HT-1080	IC₅₀	2.1 nM Compound: 58	Antiproliferative activity against human HT1080 cells assessed as cell viability after 72 hrs Antiproliferative activity against human HT1080 cells assessed as cell viability after 72 hrs	[PMID: 23859118]
MIA PaCa-2	IC₅₀	7 nM Compound: 4	Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
MIA PaCa-2	IC₅₀	7.4 nM Compound: 58	Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 72 hrs Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 72 hrs	[PMID: 23859118]
PC-3	EC₅₀	1.1 nM Compound: 4	Inhibition of NAMPT in human PC3 cells assessed as reduction in NAD level after 48 hrs by mass spectrometry Inhibition of NAMPT in human PC3 cells assessed as reduction in NAD level after 48 hrs by mass spectrometry	[PMID: 24021463]
PC-3	IC₅₀	2.7 nM Compound: 58	Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs	[PMID: 23859118]
PC-3	IC₅₀	3 nM Compound: 4	Antiproliferative activity against human PC3 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human PC3 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
RF/6A	IC₅₀	4 nM Compound: 4	Cytotoxicity against rhesus monkey RF/6A cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Cytotoxicity against rhesus monkey RF/6A cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
U-251	IC₅₀	1.8 nM Compound: 58	Antiproliferative activity against human U251 cells assessed as cell viability after 72 hrs by SRB assay Antiproliferative activity against human U251 cells assessed as cell viability after 72 hrs by SRB assay	[PMID: 23859118]

In Vitro

The activity ofGNE-617 hydrochloride is evaluated on a panel 53 non-small cell lung cancer (NSCLC) cell lines in the presence or absence of 10 μM nicotinic acid. GNE-617 inhibits NAMPT IC50 of 18.9 nM in A549 cell.The majority of cell lines exhibit a steep dose response to GNE-617 when evaluated by decrease in ATP or total nucleic acid, and the cytotoxicity is completely rescued by simultaneous addition of nicotinic acid. The majority of the cell lines tested have IC₅₀ values below 100 nM, with approximately half with IC₅₀ values less than 10 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In rats, GNE-617 (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; however, the different study durations between GNE-617 and GMX-1778 do not allow for direct comparison of retinal toxicity^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1362154-70-8
Appearance Solid
Molecular Weight 427.42
Formel C₂₁H₁₅F₂N₃O₃S
Color White to off-white
SMILES

O=C(NCC1=CC=C(S(C2=CC(F)=CC(F)=C2)(=O)=O)C=C1)C3=CN4C(C=C3)=NC=C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

All Cell Proliferation/Viability Assay

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Journal Impact Factor

Nat Commun

Niacin restriction with NAMPT-inhibition is synthetic lethal to neuroendocrine carcinoma. [Abstract]

2023 Dec 13;14(1):8095. PMID: 38092728
Cell Death Dis

Targeting metabolic vulnerability by combining NAMPT inhibitors and disulfiram for treatment of recurrent ovarian cancer. [Abstract]

2025 Apr 25;16(1):342. PMID: 40280967
Genomics

Genomic and tumor biological aspects of the anticancer nicotinamide phosphoribosyltransferase inhibitor FK866 in resistant human colorectal cancer cells. [Abstract]

2019 Dec;111(6):1889-1895. PMID: 30582964
Research Square Preprint

2024 Apr 12.
Research Square Preprint

2023 Nov 14.
Patent

US20180263995A1.
Oncotarget

Cross resistance to diverse anticancer nicotinamide phosphoribosyltransferase inhibitors induced by FK866 treatment. [Abstract]

2018 Mar 27;9(23):16451-16461. PMID: 29662658

GNE-617 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Mar 27;9(23):16451-16461. [Abstract]

Drug sensitivities of HCT116R^FK866 and HCT116 in the colony formation assay. HCT116R^FK866 and HCT116 cells are treated with 100 nM each of FK866, CHS-828, GNE-617, STF-118804, and incubated for 10 days.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 16.67 mg/mL (39.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3396 mL

11.6981 mL

23.3962 mL

5 mM

0.4679 mL

2.3396 mL

4.6792 mL

10 mM

0.2340 mL

1.1698 mL

2.3396 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.67 mg/mL (3.91 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.67 mg/mL (3.91 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Animal Weight (Per Animal) Animal Weight (Per Animal)
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Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Rats^[2]
Male naïve Sprague Dawley rats are administered once daily (QD) via oral gavage either (1) GNE-617 at 30 mg/kg for 2 consecutive days in combination with NA at 75 mg/kg twice daily (BID; 6 h apart); (2) GNE-618 at 30 mg/kg for 1 day; or (3) GMX-1778 at 30 mg/kg for 1 day. Dose selection for each compound is based on tolerability and toxicity findings from the safety studies and for nicotinic acid (NA) on the highest concentration of NA that could be administered to rats in a solution form. Formulating NA at higher concentration resulted in a suspension, and NA is determined to be unstable in a suspension form. GNE-617, GNE-618, and GMX-1778 are formulated as a solution in the vehicle of 60% polyethylene glycol (PEG 400)/10% ethanol/30% 5% dextrose in water (D5W) (vol/vol/vol), and NA is formulated as a solution in water. At 1 h and 6.5 h post-dose (on Day 2 for GNE-617), rats (3-4 rats per time point) are euthanized, and the blood, retina, and brain are collected. Blood samples are collected into K₂EDTA Microtainer tubes. The tubes are chilled on wet ice until centrifugation within 30 min of collection. Plasma is collected and transferred to 1.2 mL cluster tubes. Tissues are rinsed with phosphate-buffered saline and blotted dry using gauze. All samples are stored at more than −80°C until compound analysis. Results are expressed as an absolute concentration in retina, brain, or plasma and as a ratio of retina:plasma concentration.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3396 mL	11.6981 mL	23.3962 mL	58.4905 mL
	5 mM	0.4679 mL	2.3396 mL	4.6792 mL	11.6981 mL
	10 mM	0.2340 mL	1.1698 mL	2.3396 mL	5.8490 mL
	15 mM	0.1560 mL	0.7799 mL	1.5597 mL	3.8994 mL
	20 mM	0.1170 mL	0.5849 mL	1.1698 mL	2.9245 mL
	25 mM	0.0936 mL	0.4679 mL	0.9358 mL	2.3396 mL
	30 mM	0.0780 mL	0.3899 mL	0.7799 mL	1.9497 mL

Keywords

GNE-617

7 Cited Publications

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GNE-617

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Human Metabolite Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) GNE-617

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE-617

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Human Metabolite Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) GNE-617

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE-617 Related Classifications

HY-15766 Related Classifications