KPT-9274 CAS NO.1643913-93-2

     KPT-9274 attenuates the PAK4/β-catenin pathway, results in NAD depletion, and attenuates viability, invasion, and migration in several RCC cell lines. Inhibition of NAMPT in a cell-free enzymatic assay using recombinant NAMPT shows an IC50 of approximately 120 nM for KPT-9274. KPT-9274 attenuates G2–M transit and induces apoptosis in RCC cell lines[2].KPT-9274 demonstrates a decrement of xenograft growth comparable with that of sunitinib. There are minimal KPT-9274 effects on the normal human RPTECs and no apparent toxicity in vivo. KPT-9274 is currently being investigated in a phase I human clinical trial of patients with advanced solid malignancies and NHL[2].