TABLE 4

The calculated V_max values for the formation of primary oxidative metabolites in the incubation of [¹⁴C]dasatinib with HLM and human cDNA-expressed CYP3A4

		Determination of V_max^a^,^b
Enzymes and Metabolites			2 μM			10 μM			20 μM	Mean V_max	V_max/K_m
Enzymes and Metabolites				V	V_max	V	V_max	V	V_max	Mean V_max	V_max/K_m
								mean ± S.D.
HLM	M4	15.7	1175	129	14550	165	18599	11441 ± 8781	0.68
	M5	30.3	1231	132	1178	194	963	1124 ± 116	14.2^c
	M20	212	407	287	553	288	553	505 ± 85	3.6
	M24	10.2	53	30.3	158	52.2	272	161 ± 109	0.26
CYP3A4	M4	0.27	16	1.96	111	2.65	149	92 ± 69	0.82
	M20	1.68	11	9.25	37	9.69	39	29 ± 16	4.8
	M24	0.30	1.9	0.59	3.7	1.05	6.6	4.0 ± 2.3	0.4

↵ a The unit for V and V_max was pmol/mg protein/min for HLM and pmol/pmol P450/min for CYP3A4. CYP3A4 content used was 76 pmol/mg in HLMs (Rostami-Hodjegan and Tucker, 2007). The unit for V_max/K_m was μl/min/pmol CYP3A4 for M4, M20, and M24.
↵ b The K_m values used for calculations were from Table 3.
↵ c The unit of V_max/K_m for M5 was μl/min/mg proteins for M5.