Name | KPT9274 |
Description | KPT9274 (PAK4-IN-1) is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule. |
Cell Research | 786-0, ACHN, Caki-1 and U-2 OS cells are treated with KPT-9274 (1 μM and 5 μM) incubating for 12 hours. |
Animal Research | 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. |
In vitro | 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 vivo | In mice, KPT-9274 (200 mg/kg) daily is administered either intravenously or orally with the absence of any signs of toxicity. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 55 mg/mL (90.07 mM)
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Keywords | KPT9274 |
Inhibitors Related | Fingolimod hydrochloride | GNE-617 | Nampt activator-2 | PF-3758309 hydrochloride | G-5555 | FRAX1036 | Nampt-IN-1 | FRAX597 | 5-Aminosalicylic Acid | Fingolimod | Nampt activator-1 | (E)-Daporinad |
Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |