YAP/TAZ inhibitor-2

Names

[ Name ]:
YAP/TAZ inhibitor-2

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Stem Cell/Wnt >> YAP

[Target]

EC50: 3 nM (TEAD-YAP/TAZ)[1]

[In Vitro]

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].

[In Vivo]

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].

[References]

[1]. Xu, xiaofeng, et al. Bicyclic compounds, compositions and use thereof. WO2022037568A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₄F₄N₄O

[ Molecular Weight ]:
390.33

YAP/TAZ inhibitor-2

Names

Biological Activity

Chemical & Physical Properties

Related Compounds