CDK8-IN-11

• CAT Number: I042818
• CAS Number: 2839338-28-0
• Molecular Formula: C19H15F3N4O2
• Molecular Weight: 388.34
• Purity: ≥95%
• Synonyms: 1-[4-(6-aminopyridin-3-yl)oxyphenyl]-3-[3-(trifluoromethyl)phenyl]urea
• InChI: InChI=1S/C19H15F3N4O2/c20-19(21,22)12-2-1-3-14(10-12)26-18(27)25-13-4-6-15(7-5-13)28-16-8-9-17(23)24-11-16/h1-11H,(H2,23,24)(H2,25,26,27)
• InChIKey: MBIXOXMOHXFUFZ-UHFFFAOYSA-N
• SMILES: C1=CC(=CC(=C1)NC(=O)NC2=CC=C(C=C2)OC3=CN=C(C=C3)N)C(F)(F)F

CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer[1].
CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6% [1].
CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells[1].
CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM, 24 h) suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells[1].
CDK8-IN-11 (0.5-2 μM, 48 h) increases the number of cells in the G1 phase in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM) reverses Sorafenib (HY-10201) resistance of HCT-116 cells[1].
CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice[1].
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days[1].
CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10−6 cm/s[1].

Reference

[1]. Yao Yao Yan, et al. Design and Synthesis of a 2-Amino-pyridine Derivative as a Potent CDK8 Inhibitor for Anti-colorectal Cancer Therapy. J Med Chem. 2022 Sep 20.
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