Powder: -20°C for 3 years
In solvent: -80°C for 2 years
KPT-9274 is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.
Description | KPT-9274 is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule. |
Targets&IC50 | NAMPT:~120 nM |
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. |
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. |
Synonyms | KPT-9274, PAK4-IN-1, KPT 9274 |
Molecular Weight | 610.637 |
Formula | C35H29F3N4O3 |
CAS No. | 1643913-93-2 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 32 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
KPT9274 1643913-93-2 代谢 细胞骨架 PAK NAMPT KPT 9274 PAK4-IN-1 KPT-9274 Inhibitor inhibitor inhibit