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. Author manuscript; available in PMC: 2019 Sep 1.
Published in final edited form as: Clin Cancer Res. 2018 Dec 5;25(5):1601–1611. doi: 10.1158/1078-0432.CCR-18-0919

Table 1.

Pharmacokinetic parameters of the developed LSD1 inhibitors*

S2116 S2157
graphic file with name nihms-1515965-t0001.jpg graphic file with name nihms-1515965-t0002.jpg
(±)-trans (±)-trans
Cmax (μM) 3.77 ± 0.56 4.33 ± 3.07
T1/2 (h) 10.88 ± 2.97 0.88 ± 0.04
AUC (μM•h) 41.78 ± 8.66 5.75 ± 3.67
nAUC (μM•h)** 0.84 ± 0.17 0.11 ± 0.07
Plasma concentration at 0.5 h (μM) 8.17 ± 2.80 5.71 ± 2.47
Brain concentration at 0.5 h (μmol/kg) 1.35 ± 0.39 64.0 ± 3.46
Brain/Plasma ratio 0.17 ± 0.03 13.0 ± 6.26
*

Pharmacokinetic parameters were determined in NOD.CB17-PrkdcSCID/J mice treated with a single intraperitoneal injection of either S2116 or S2157 in 5 mL of 6.25% DMSO-saline at 50 mg/kg (n = 3).

**

Dose-normalized AUC