CDK8-IN-1

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

Research Areas >> Cancer

CDK8:3 nM (IC50)

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].

Mice[1] CDK8-IN-1 is administrated to mice with 5 mg/kg, 25mg/mg 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.

Abemaciclib(LY2835219) | Ribociclib (LEE011) | Dinaciclib (SCH727965) | THZ1 2HCl | Roscovitine (CYC202) | THZ531 | RO-3306 | Flavopiridol | NVP 2 | BAY-1143572 Racemate | CYC-065 | AZD5438 | BIO | Kenpaullone | SNS-032 (BMS-387032)