CDK8-IN-16

• Description :

  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].

• 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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  CDK19; CDK8