Cat. No.: HY-12628

GNE-618

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC₅₀ of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.

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Pureté: 99.89%
CAS No.: 1362151-42-5
Formule: C₂₁H₁₅F₃N₄O₃S
Masse moléculaire:460.43

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GNE-618 Chemical Structure

CAS No.: 1362151-42-5

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 6 nM (NAMPT)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.0043 μM Compound: 26	Antiproliferative activity against human A2780 cells assessed as cell viability after 72 hrs by SRB assay Antiproliferative activity against human A2780 cells assessed as cell viability after 72 hrs by SRB assay	[PMID: 24021463]
A2780	IC₅₀	0.004 μM Compound: 3; GNE-618	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]
B16-F10	IC₅₀	>1000 nM Compound: 26	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	21 nM Compound: 26	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	501 nM Compound: 26	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	863 nM Compound: 26	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	8 nM Compound: 26	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]
HT-1080	IC₅₀	9 nM Compound: 26	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]
MIA PaCa-2	IC₅₀	30 nM Compound: 26	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]
PC-3	EC₅₀	1.2 nM Compound: 26	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	9 nM Compound: 26	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	386 nM Compound: 26	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]

In Vitro

GNE-618 reduces levels of NAD with an EC₅₀ of 2.6 nM in the NSCLC cell line Calu-6^[1].
? GNE-618 (10-30 nM; 72 hours) reveals an increase in the sub-2N population and a decreases in the percentage of cells in the G1 and M phases of the cell cycle in Calu-6 cells^[1].
? GNE-618 also reduces cellular proliferation of Calu-6 cells as determined using two different assay formats, either measuring ATP (EC₅₀ of 13.6 ± 1.8 nM) or total protein content (SRB assay; EC₅₀ of 25.8 ± 4.2 nM)^[1]

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

In Vivo

GNE-618 (100 mg/kg; p.o.; twice daily for 5 days) significantly inhibits tumor growth by 88% and has minimal effects on body weight in STO#81 patient-derived gastric model^[1].

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

Chemical Information

CAS No. 1362151-42-5
Appearance Solid
Masse moléculaire 460.43
Formule C₂₁H₁₅F₃N₄O₃S
Color Off-white to light yellow
SMILES

O=C(NCC1=CC=C(S(=O)(C2=CC(C(F)(F)F)=CC=C2)=O)C=C1)C3=CC(C=NN4)=C4N=C3
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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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
Research Square Preprint

2024 Apr 12.

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (271.49 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

2.1719 mL

10.8594 mL

21.7188 mL

5 mM

0.4344 mL

2.1719 mL

4.3438 mL

10 mM

0.2172 mL

1.0859 mL

2.1719 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.08 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Xiao Y, et al. Dependence of tumor cell lines and patient-derived tumors on the NAD salvage pathway rendersthem sensitive to NAMPT inhibition with GNE-618. Neoplasia. 2013 Oct;15(10):1151-60. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1719 mL	10.8594 mL	21.7188 mL	54.2971 mL
	5 mM	0.4344 mL	2.1719 mL	4.3438 mL	10.8594 mL
	10 mM	0.2172 mL	1.0859 mL	2.1719 mL	5.4297 mL
	15 mM	0.1448 mL	0.7240 mL	1.4479 mL	3.6198 mL
	20 mM	0.1086 mL	0.5430 mL	1.0859 mL	2.7149 mL
	25 mM	0.0869 mL	0.4344 mL	0.8688 mL	2.1719 mL
	30 mM	0.0724 mL	0.3620 mL	0.7240 mL	1.8099 mL
	40 mM	0.0543 mL	0.2715 mL	0.5430 mL	1.3574 mL
	50 mM	0.0434 mL	0.2172 mL	0.4344 mL	1.0859 mL
	60 mM	0.0362 mL	0.1810 mL	0.3620 mL	0.9050 mL
	80 mM	0.0271 mL	0.1357 mL	0.2715 mL	0.6787 mL
	100 mM	0.0217 mL	0.1086 mL	0.2172 mL	0.5430 mL

Keywords

GNE-618

2 Cited Publications

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GNE-618

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GNE-618

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GNE-618

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GNE-618

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GNE-618 Related Classifications

HY-12628 Related Classifications