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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.
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $178 | 8-10 weeks | |
| 25 mg | $637 | 8-10 weeks | |
| 50 mg | $828 | 8-10 weeks | |
| 100 mg | $1,240 | 8-10 weeks | |
| 1 mL x 10 mM (in DMSO) | $183 | 8-10 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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