tcsc3207 CZC-25146

CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.

IC50 value: 4.76 nM/6.87 nM(wild type/G2019S LRRK2) [1]

Target: LRRK2

CZC-25146displayed a very clean profile, it inhibited only five kinases (PLK4, GAK, TNK1, CAMKK2 and PIP4K2C) with high potency, none of which have been classified as predictors of genotoxicity or hematopoietic toxicity. CZC-25146 neither caused cytotoxicity in human cortical neurons at concentrations below 5

μM over a seven-day treatment in culture nor did it block neuronal development in vitro. CZC-25146 possesses favorable pharmacokinetic properties, such as a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/hr/kg that render it suitable for in-vivo studies.