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GNE-618

Catalog No. T15403   CAS 1362151-42-5

GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.

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GNE-618 Chemical Structure
GNE-618, CAS 1362151-42-5
Pack Size Availability Price/USD Quantity
5 mg 8-10 weeks $ 178.00
25 mg 8-10 weeks $ 637.00
50 mg 8-10 weeks $ 828.00
100 mg 8-10 weeks $ 1,240.00
1 mL * 10 mM (in DMSO) 8-10 weeks $ 183.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.
Targets&IC50 NAMPT:6 nM
In vitro GNE-618 decreases levels of NAD (EC50: 2.6 nM in the NSCLC cell line Calu-6). GNE-618 also reduces cellular proliferation of Calu-6 cells as determined using two different assay formats, either measuring ATP (EC50: 13.6 nM) or total protein content (SRB assay; EC50: 25.8 nM). GNE-618 (10-30 nM; 72 hours) displays an increase in the sub-2N population and a reduction in the percentage of cells in the G1 and M phases of the cell cycle in Calu-6 cells.
In vivo In the STO#81 patient-derived gastric cancer model, GNE-618 administered orally at a dosage of 100 mg/kg twice daily for 5 days significantly inhibits tumor growth by 88%, while having minimal effects on body weight.
Molecular Weight 460.43
Formula C21H15F3N4O3S
CAS No. 1362151-42-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

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Keywords

GNE-618 1362151-42-5 Metabolism NAMPT GNE 618 GNE618 inhibitor inhibit

 

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