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. 2018 Jun 11;9(7):746–751. doi: 10.1021/acsmedchemlett.8b00182

Table 1. Cellular Potency, in vitro CLint, and Rat PK Data of 9, 10, and 2.

graphic file with name ml-2018-00182j_0008.jpg

  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
a

Not determined.