Table 1. Cellular Potency, in vitro CLint, and Rat PK Data of 9, 10, and 2.
9 | 10 | 2 | |
---|---|---|---|
cellular HCT116-IDH1R132H/+ (IC50/μM) | 0.56 | 0.047 | 0.014 |
in vitro liver microsomal CLint (μL/min/mg) | 34 | 101 | 588 |
in vivo plasma clearance (mL/min/kg) | n.d.a | 17 | 41 |
oral AUC (μM·h) | n.d. | 14 | 0.4 |
oral bioavailability (%) | n.d. | 67 | 4 |
Not determined.