Description
KPT-9274 is a potent, specific, dual NAMPT and PAK4 inhibitor with IC50 of 120nM (NAMPT), also is an orally bioavailable PAK4 allosteric modulator with IC50 of 30nM in MS-751 cell MTT assay; attenuates the PAK4/beta-catenin pathway, results in NAD depletion, and attenuates viability, invasion, and migration in several RCC cell lines (IC50=600nM for Caki-1 cells); attenuates G2/M transit and induces apoptosis, shows specificity for attenuation of NAD biosynthesis targets preferentially in RCC cells; decreases tumor growth in xenograft model of RCC. Blood Cancer Phase 1 Clinical