Padnarsertib (KPT-9274)

Description: This product has been discontinued. KPT-9274 (PAK4-IN-1) is a potent, selective, orally bioavailable small molecule, non-competitive dual inhibitor of PAK4/NAMPT inhibitor. KPT-9274 disrupts the PAK4/NAMPT signaling pathway, which may lead to the reduction of G2-M transit and induction of apoptosis as well as decrease in cell invasion and migration in several human RCC cell lines. Inhibition of the PAK4 signaling pathway by KPT-9274 attenuates nuclear beta-catenin as well as the Wnt/beta-catenin targets cyclin D1 and c-Myc. KPT-9274 demonstrated the expected on-target effects in a mouse model and is under a phase I clinical trial for solid tumors and lymphomas.

References: Mol Cancer Ther. 2016 Sep; 15(9):2119-29.