Drug metabolism in human hepatocytes assessed as formation of 2-(7-(3-((1R,2S)-2-aminocyclohexylamino)-6-carbamoyl-1,2,4-triazin-5-ylamino)-3-oxo-3H-indol-2-ylamino)-3-mercaptopropanoic acid by measuring parent compound level at 10 uM after 6 hrs
Metabolic stability in rat hepatocytes assessed as formation of 2-(7-(3-((1R,2S)-2-aminocyclohexylamino)-6-carbamoyl-1,2,4-triazin-5-ylamino)-3-oxo-3H-indol-2-ylamino)-3-mercaptopropanoic acid by measuring parent compound level at 10 uM after 6 hrs
Metabolic stability in dog hepatocytes assessed as formation of 2-(7-(3-((1R,2S)-2-aminocyclohexylamino)-6-carbamoyl-1,2,4-triazin-5-ylamino)-3-oxo-3H-indol-2-ylamino)-3-mercaptopropanoic acid by measuring parent compound level at 10 uM after 6 hrs
Metabolic stability in monkey hepatocytes assessed as formation of 2-(7-(3-((1R,2S)-2-aminocyclohexylamino)-6-carbamoyl-1,2,4-triazin-5-ylamino)-3-oxo-3H-indol-2-ylamino)-3-mercaptopropanoic acid by measuring parent compound level at 10 uM after 6 hrs
Cytotoxicity against C57BL/6 mouse bone marrow cells assessed as growth inhibition preincubated for 4 days followed by [3H]-thymidine addition measured after 5 hrs by betaplate counting analysis
Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis
Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimulation measured after 5 mins by flow cytometric analysis