GNE-618 (C09-1135-920)

GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC 50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activityIn VitroGNE-618 reduces levels of NAD with an EC 50 of 2.6 nM in the NSCLC cell line Calu-6. 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. GNE-618 also reduces cellular proliferation of Calu-6 cells as determined using two different assay formats, either measuring ATP (EC 50 of 13.6 ± 1.8 nM) or total protein content (SRB assay; EC 50 of 25.8 ± 4.2 nM)MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoGNE-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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.IC50& Target:IC50: 6 nM (NAMPT). Specifications and Purity: 10mM in DMSO. Molecular Formula: C21H15F3N4O3S. Molecular Weight: 460.43.