体外活性
GNE-618 decreases levels of NAD (EC50: 2.6 nM in the NSCLC cell line Calu-6). GNE-618 also reduces cellular proliferation of Calu-6 cells as determined using two different assay formats, either measuring ATP (EC50: 13.6 nM) or total protein content (SRB assay; EC50: 25.8 nM). GNE-618 (10-30 nM; 72 hours) displays an increase in the sub-2N population and a reduction in the percentage of cells in the G1 and M phases of the cell cycle in Calu-6 cells.
体内活性
In STO#81 patient-derived gastric model, 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.
Cas No.
1362151-42-5
分子式
C21H15F3N4O3S
分子量
460.43
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years