YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity[1].
YAP/TAZ inhibitor-2 (compound 5) (0-20000 nM; 24 h) shows antiproliferative activity with an IC50 value of 5.33 nM in NCI-H226 cells[1].
YAP/TAZ inhibitor-2 (0.5, 2, 5, 50 mg/kg; p.o.; daily for 28 days) shows anti-tumor activity with no significant body weight loss during the treatment in BALB/c nude mice (NCI-H226 xenograft model)[1].
[1]. Xu, xiaofeng, et al. Bicyclic compounds, compositions and use thereof. WO2022037568A1.
