Inhibition of human CSF1R tyrosine kinase domain (538 to 972 residues) using Poly(Glu, Tyr)-biotinylated peptide as substrate preincubated for 5 mins followed by substrate addition and measured after 10 mins by HTRF assay
Inhibition of CSF1R in CSF1-induced DBA/1J mouse BMMC assessed as reduction in LPS-induced IL6 production preincubated for overnight followed by LPS-stimulation and measured after 6 hrs by ELISA
Stability in human liver S9 fraction assessed as parent compound remaining at 5 uM preincubated for 5 mins followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis
Stability in Sprague-Dawley rat liver S9 fraction assessed as parent compound remaining at 5 uM preincubated for 5 mins followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis
Stability in CD-1 mouse liver S9 fraction assessed as parent compound remaining at 5 uM preincubated for 5 mins followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis
Invivo inhibition of CSF1R in CSF1-induced DBA/1J mouse assessed as reduction in LPS-induced IL6 production at 10 mg/kg, po treated for 1 hr prior to CSF1-stimulation followed by LPS-addition and measured after 2 hrs by ELISA relative to control
Invivo inhibition of CSF1R in CSF1-induced DBA/1J mouse assessed as reduction in LPS-induced IL6 production at 10 mg/kg, po treated for 6 hrs prior to CSF1-stimulation followed by LPS-addition and measured after 2 hrs by ELISA relative to control