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GNE-618

GNE-618
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.
Catalog No. T15403Cas No. 1362151-42-5
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GNE-618

Catalog No. T15403Cas No. 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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Pack SizePriceAvailabilityQuantity
5 mg$1788-10 weeks
25 mg$6378-10 weeks
50 mg$8288-10 weeks
100 mg$1,2408-10 weeks
1 mL x 10 mM (in DMSO)$1838-10 weeks
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight460.43
FormulaC21H15F3N4O3S
Cas No.1362151-42-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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