CDK8-IN-1

Product NameCDK8-IN-1
CAS1629633-48-2
MFC11H8F3N3O
MW255.2
EINECS
MOL File1629633-48-2.mol

Chemical Properties

Boiling point	406.2±45.0 °C(Predicted)
Density	1.429±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Solid
pka	12.46±0.50(Predicted)
color	White to light brown

Usage And Synthesis

Description

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].

Uses

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

in vivo

CDK8-IN-1 displays low systemic clearance, very good exposure and oral bioavailability. The t_max is 0.25 h by PO. The mean values of C_max 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].

IC 50

CDK8: 3 nM (IC₅₀)

References

[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.