YTP-17 is an orally active YAP-TEAD protein-protein interaction inhibitor with an IC50 of 4 nM. YTP-17 shows anti-tumor efficacy.
YTP-17 shows antiproliferative activity against NCI-H2052 cells with an IC50 of 45 nM[1].
YTP-17 (60 mg/kg; oral gavage; once daily; for 2 weeks) shows anti-tumor efficacy in NCI-H226 xenograft mouse model[1].
References:
[1]. Holger Sellner, et al. Optimization of a Class of Didrobenzofurane Analogs toward Orally Efficacious YAP-TEAD Protein-Protein Interaction Inhibitors. ChemMedChem. 2023 Jun 1;18(11):e202300051.