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.
IC50&Target
IC50: 6 nM (NAMPT)
体外研究
GNE-618 reduces levels of NAD with an EC50 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 (EC50 of 13.6 ± 1.8 nM) or total protein content (SRB assay; EC50 of 25.8 ± 4.2 nM)
体内研究
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.
分子式
C21H15F3N4O3S
分子量
460.43
CAS号
1362151-42-5
运输条件
Room temperature in continental US; may vary elsewhere.