Padnarsertib, also known as KPT-9274 and PAK4-IN-1, is a potent, selective and dual PAK4/NAMPT inhibitor. KPT-9274 interferences with PAK4/NAMPT signaling pathways, which results in reduction of G2-M transit as well as induction of apoptosis and decrease in cell invasion and migration in several human RCC cell lines. Mechanistic studies demonstrate that 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. KPT-9274 demonstrated the expected on-target effects in this mouse model. KPT-9274 is being evaluated in a phase I human clinical trial in solid tumors and lymphomas, which will allow this data to be rapidly translated into the clinic for the treatment of RCC.
Cat.No
DC74683
Name
KPT-9274
Chemical Properties
CAS
1643913-93-2
Formula
C35H29F3N4O3
MW
610.637
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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