AZ13705339 hemihydrate is a highly potent and selective PAK1 inhibitor with IC 50 s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 hemihydrate has binding affinities to PAK1 and PAK2 , with K d s of 0.28 nM and 0.32 nM, respectively. AZ
In Vitro:AZ13705339 (1 μM) hemihydrate inhibits αIgM-controlled adhesion and not PMA-induced adhesion in Namalwa cells. AZ13705339 (300 nM, 30 min) prevents Siglec-8 engagement-induced eosinophil death. MCE has not independently confirmed the accuracy of
In Vivo:AZ13705339 hemihydrate (100mg/kg, P.O.) has moderate clearance and oral C max of 7.7 μM in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Biological Activity:AZ13705339 hemihydrate is a highly potent and selective PAK1 inhibitor with IC 50 s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 hemihydrate has binding affinities to PAK1 and PAK2 , with K d s of 0.28 nM and 0.32 nM, respectively. AZ