1362151-42-5

1362151-42-5 structure
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: 2025-08-26 10:30:23
  • 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

[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.

Molecular Formula C21H15F3N4O3S
Molecular Weight 460.43
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