Cat No:LP000339
Product Name:KPT-9274
CAS#1643913-93-2
KPT-9274 is a dual inhibitor of nicotinamide phosphoribosyltransferase (NAMPT; IC50 = 120 nM) and the serine/threonine protein kinase PAK4.1 It selectively inhibits the phosphorylation of PAK4 in renal cell carcinoma cells over normal renal tubular epithelium, and U2OS cells with a PAK4 knockout exhibit a 6-fold resistance to growth inhibition by KPT-9274. KPT-9274 inhibits growth and decreases invasion and migration of renal cell carcinoma cell lines in a dose-dependent manner. Oral administration of KPT-9274 (100 mg/kg) reduces tumor growth in a 786-O renal carcinoma mouse xenograft model comparable to sunitinib (Item No. 13159). It also reduces tumorigenesis in MDA-MB-231, MDA-MB-468, and SUM159 mouse xenograft models of triple-negative breast cancer.
