TABLE 1 Enzyme kinetic parameters for the formation of M7 in incubations of brivanib with HLM, cDNA-expressed CYP3A4, and cDNA-expressed CYP1A2
Incubations were conducted at 37°C with HLM (0.1 mg protein/ml), CYP3A4 (25 pmol/ml), or CYP1A2 (10 pmol/ml) in the presence of NADPH. Enzyme kinetic parameters were estimated by fitting the data to the Michaelis-Menten equation using a nonlinear regression analysis with GraphPad Prism (version 5.04; GraphPad Software Inc.). The corresponding r2 values for the curves ranged from 0.90 to 0.94.