GNE-618 is a potent, selective NAMPT inhibitor with IC50 of 6 nM, depletes NAD and induces cell death in vitro and in vivo.
GNE-618 reduced levels of NAD with an 50% minimal response (EC50) of 2.6 nM in the NSCLC cell line Calu-6, reduced cellular proliferation of Calu-6 cells with IC50 of 13. 6 nM.
NAMPT, but not NAPRT1, mRNA and protein levels inversely correlate with sensitivity to GNE-618 across a panel of 53 non-small cell lung carcinoma cell lines.
GNE-618 inhibits in vivo tumor growth in an A549 non-small cell lung carcinoma (NSCLC) model.
