GNE-617
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.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 1362154-70-8
- Formula: C21H15F2N3O3S
- Molecular Weight:427.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GNE-617
More- Nat Commun. 2023 Dec 13;14(1):8095. [Abstract]
- Cell Death Dis. 2025 Apr 25;16(1):342. [Abstract]
- Genomics. 2019 Dec;111(6):1889-1895. [Abstract]
- Research Square Preprint. 2024 Apr 12.
- Research Square Preprint. 2023 Nov 14.
- Patent. US20180263995A1.
- Oncotarget. 2018 Mar 27;9(23):16451-16461. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
Biological Activity
IC50: 5 nM (NAMPT)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.002 μM
Compound: 1; GNE-617
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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
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[PMID: 27541271] |
| A2780 | IC50 |
0.002 μM
Compound: 58
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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
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[PMID: 23859118] |
| B16-F10 | IC50 |
71 nM
Compound: 4
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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
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[PMID: 24021463] |
| Calu-6 | IC50 |
5 nM
Compound: 4
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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
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[PMID: 24021463] |
| COS-1 | IC50 |
5 nM
Compound: 4
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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
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[PMID: 24021463] |
| COS-7 | IC50 |
9 nM
Compound: 4
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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
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[PMID: 24021463] |
| HCT-116 | IC50 |
2 nM
Compound: 4
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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
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[PMID: 24021463] |
| HCT-116 | IC50 |
2 nM
Compound: 58
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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
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[PMID: 23859118] |
| HT-1080 | IC50 |
2 nM
Compound: 4
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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
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[PMID: 24021463] |
| HT-1080 | IC50 |
2.1 nM
Compound: 58
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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
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[PMID: 23859118] |
| MIA PaCa-2 | IC50 |
7 nM
Compound: 4
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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
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[PMID: 24021463] |
| MIA PaCa-2 | IC50 |
7.4 nM
Compound: 58
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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
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[PMID: 23859118] |
| PC-3 | EC50 |
1.1 nM
Compound: 4
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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
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[PMID: 24021463] |
| PC-3 | IC50 |
2.7 nM
Compound: 58
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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
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[PMID: 23859118] |
| PC-3 | IC50 |
3 nM
Compound: 4
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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
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[PMID: 24021463] |
| RF/6A | IC50 |
4 nM
Compound: 4
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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
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[PMID: 24021463] |
| U-251 | IC50 |
1.8 nM
Compound: 58
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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
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[PMID: 23859118] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1362154-70-8
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Appearance Solid
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Molecular Weight 427.42
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Formula C21H15F2N3O3S
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Color White to off-white
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SMILES
O=C(NCC1=CC=C(S(C2=CC(F)=CC(F)=C2)(=O)=O)C=C1)C3=CN4C(C=C3)=NC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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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 -
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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 HCT116RFK866 and HCT116 in the colony formation assay. HCT116RFK866 and HCT116 cells are treated with 100 nM each of FK866, CHS-828, GNE-617, STF-118804, and incubated for 10 days.
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
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.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
GNE-617 Related Classifications
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