Description
InformationPLX5622 PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3.TargetsCSF-1R (Cell-free assay); FLT3 (Cell-free assay); KIT (Cell-free assay); AURKC (Cell-free assay); KDR (Cell-free assay);0.016 µM; 0.39 µM; 0.86 µM; 1 µM; 1.1 µMIn vivoIn vivo PLX5622 demonstrates desirable PK properties in mice, rats, dogs, and monkeys, with a brain penetrance of ~20%. PLX5622 has low systemic clearance, moderate volume of distribution, and favorable oral bioavailability (F > 30%) in all four species. PLX5622 is a useful compound for investigating microglial dynamics. It allows for the sustained and specific elimination of microglia, preceding and during pathology development of Alzheimer’s disease (AD). Long-term PLX5622-mediated microglial depletion is highly robust, sustainable, and specific to the microglial compartment