1362151-42-5
1362151-42-5 structure
- Name: GNE-618
- Chemical Name: GNE-618
- CAS Number: 1362151-42-5
- Molecular Formula: C21H15F3N4O3S
- Molecular Weight: 460.43
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Nampt
- Create Date: 2019-12-07 14:49:54
- Modify Date: 2024-02-26 12:37:01
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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[1].
| Name | GNE-618 |
|---|
| Description | 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[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 6 nM (NAMPT)[1] |
| 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] |
| 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]. |
| References |
| Molecular Formula | C21H15F3N4O3S |
|---|---|
| Molecular Weight | 460.43 |