CDK8-IN-1

• CAT Number: I046272
• CAS Number: 1629633-48-2
• Molecular Formula: C11H8F3N3O
• Molecular Weight: 255.20
• Purity: ≥95%
• Synonyms: 4-pyridin-4-yl-3-(trifluoromethyl)-1H-pyrrole-2-carboxamide
• InChI: InChI=1S/C11H8F3N3O/c12-11(13,14)8-7(5-17-9(8)10(15)18)6-1-3-16-4-2-6/h1-5,17H,(H2,15,18)
• InChIKey: RKTPHHQXNCHBCF-UHFFFAOYSA-N
• SMILES: C1=CN=CC=C1C2=CNC(=C2C(F)(F)F)C(=O)N

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].

Reference

[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.
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