Animal experiment:

Mice[1]CDK8-IN-1 is administrated to mice with 5 mg/kg, 25mg/mg by IV and PO respectively[1].

CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.

CDK8-IN-1 displays low systemic clearance, very good exposure and oral bioavailability. The tmax is 0.25 h by PO. The mean values of Cmax are 9940 μg/L, 12740 μg/L by IV and PO respectively. The values of AUC are 9378, 25952 by IV and PO respectively[1].

[1]. Han X, et al. Discovery of potent and selective CDK8 inhibitors through FBDD approach. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4488-4492.