AN1025 is an oral small molecule β-catenin suppressor, which is currently in the lead optimization phase.

Wnt/β-catenin pathway is one of the key tumor-promoting signaling cascades that regulate cell cycle progression, epithelial-mesenchymal transition, angiogenesis, stemness, and tumor immune microenvironment. Aberrant activation of Wnt signaling as a result of genetic mutation has been linked to different cancers. Therefore, this pathway represents a promising target for therapeutic intervention.

In our preclinical studies, AN1025 treatment led to the reduction of β-catenin (a key component in Wnt signaling pathway) level in tumor cells. In addition, human cancer cell lines with high β-catenin expression were more sensitive to AN1025, when compared with those having low β-catenin expression, suggesting that β-catenin could serve as a biomarker of sensitivity to AN1025.

AN1025 showed dose-dependent anti-tumor activities in colo205 xenograft mice models.