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GNE-618

Names

[ CAS No. ]:
1362151-42-5

[ Name ]:
GNE-618

Biological Activity

[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]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Nampt

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H15F3N4O3S

[ Molecular Weight ]:
460.43

Related Compounds