LSN3154567 is a novel potent, highly selective, competitive NAMPT inhibitor with IC50 of 3.1 nM.
LSN3154567 exhibit no significant activity against the CEREP Kinase panel except CSF1R (IC50=0.84 uM).
LSN3154567 exhibits a broad spectrum of anti-cancer activity against different types of cancer cell lines, exhibits a dose-dependent inhibition of NAD+ formation with TED50 of 2 mg/kg in A2780 tumor xenograft models.
LSN3154567 also exhibits robust efficacy in multiple tumor models deficient in NAPRT1, does not cause observable retinal and hematological toxicities in the rodents when coadministered with nicotinic acid (NA).
