CDK8-IN-16

CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%[1].

Product Specifications

CAS Number

[1860885-61-5]

UNSPSC

12352005

Target

CDK; STAT; Wnt

Related Pathways

Cell Cycle/DNA Damage; JAK/STAT Signaling; Stem Cell/Wnt

Field of Research

Cancer

Smiles

O=C(N1CC(C1)OC)C2=NC3=C(C4=CC=C(C5=CN(C)N=C5)C=C4)C=NC(N)=C3C=C2

Molecular Formula

C23H22N6O2

Molecular Weight

414.46

References & Citations

[1]Mallinger A, et al., 2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. ACS Med Chem Lett. 2016 Mar 28;7 (6) :573-8.