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. AZ13705339 hemihydrate can be used in the research of cancers.
性状
Solid
IC50 & Target[1][2]
PAK2 0.32 nM (Kd) PAK1 0.28 nM (Kd)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
AZ13705339 hemihydrate (100 mg/kg, P.O.) has moderate clearance and oral C max of 7.7 μM in rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. McCoull W, et al. Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. ACS Med Chem Lett. 2016;7(12):1118-1123. Published 2016 Sep 14. [2]. Martin F M de Rooij, et al. A loss-of-adhesion CRISPR-Cas9 screening platform to identify cell adhesion-regulatory proteins and signaling pathways. Nat Commun. 2022 Apr 19;13(1):2136.
溶解度数据
In Vitro: DMSO : 100 mg/mL (156.55 mM; Need ultrasonic)配制储备液