KPT9274 是一种非竞争性的 PAK4 和 NAMPT 双重抑制剂（IC50= ~120 nM）。它是一种口服生物可利用的小分子。

KPT-9274 is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.

In several human RCC cell lines, KPT-9274 interferences with PAK4 and NAD biosynthetic pathways leading to reduction of G2/M transit as well as induction of apoptosis and decrease in cell invasion and migration. The inhibition of the PAK4 pathway by KPT-9274 attenuates nuclear β-catenin as well as the Wnt/β-catenin targets cyclin D1 and c-Myc.

In mice, KPT-9274 (200 mg/kg) daily is administered either intravenously or orally with the absence of any signs of toxicity.

786-0, ACHN, Caki-1 and U-2 OS cells are treated with KPT-9274 (1 μM and 5 μM) incubating for 12 hours.

786-O (VHL-mut) human RCC xenograft model (nude mice) is treated with KPT-9274 (100 and 200 mg/kg),prepared in 58% Polyvinylpyrrolidone K30 + 21% methyl cellulose + 21% Phospholipon 90 g, by oral gavage.

1643913-93-2

C35H29F3N4O3

610.637

KPT 9274;PAK4-IN-1;KPT-9274

DMSO:32 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years