CAS 3027484-09-6

Fórmula: C19H16F3NO

InChI: InChI=1S/C19H16F3NO/c1-2-18(24)23-10-9-14-3-4-15(11-16(14)12-23)13-5-7-17(8-6-13)19(20,21)22/h2-8,11H,1,9-10,12H2

Clave InChI: BTKHMDKDDHZABJ-UHFFFAOYSA-N

SMILES: C=CC(=O)N1CCC2=C(C1)C=C(C=C2)C3=CC=C(C=C3)C(F)(F)F

pan-TEAD-IN-1

CAS: 3027484-09-6

pan-TEAD-IN-1 (Compound 3) is an orally active pan-inhibitor of TEAD, disrupting its interaction with coactivators YAP/TAZ by targeting the palmitoylation site of TEAD. This inhibition leads to the downregulation of oncogene transcription, such as Ctgf and Cyr61, within the Hippo signaling pathway. Demonstrating outstanding efficacy, pan-TEAD-IN-1 has an IC₅₀ of 0.36 nM for luciferase and 1.52 nM for H226 cells, along with favorable pharmacokinetic properties (AUC0–∞= 228.7 μg/mL·min, T1/2= 183.9 min). The compound significantly inhibits tumor growth in xenograft models of TEAD-dependent cancers, indicating its potential for research in these cancer types.

Fórmula: C₁₉H₁₆F₃NO

Forma y color: Solid

Peso molecular: 331.33

Ref: TM-T203500