Description
A potent and specific small-molecule Porcupine (PORCN) inhibitor with IC50 of 1nM in the PORCN radioligand binding assay; potently inhibits Wnt signaling with IC50 of 0.4nM, with no major cytotoxicity; reduces Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2; is potent and efficacious in multiple tumor models at well-tolerated doses in vivo. Colon Cancer Phase 2 Clinical