TABLE 1

Inhibition of thiamine uptake by JAKi and other xenobiotics

Values represent the mean ± S.D. of triplicate determinations in a representative experiment of three independent experiments.

IC50 Value for Thiamine Uptake
CompoundCaco-2THTR-1THTR-2
µMµMµM
Fedratinib0.940 ± 0.0807.10 ± 1.261.36 ± 0.59
AZD1480183 ± 68.922.2 ± 6.2015.3 ± 2.90
Cerdulatinib>300276 ± 117>300
Momelotinib>30.0>30.0>30.0
Trimethoprim154 ± 22.46.84 ± 1.685.56 ± 0.65
Oxythiamine198 ± 16.067.3 ± 7.5066.4 ± 21.4
Amprolium9.40 ± 2.802.60 ± 0.930.620 ± 0.270