β-catenin-IN-6 is a β-catenin inhibitor, targeting to canonical Wingless-related integration site signaling pathway. β-catenin-IN-6 inhibits human colorectal cancer cells proliferation, as well as in a β-catenin/RK3E mouse model.
β-catenin-IN-6 (compound 9) (24 h) inhibits in LoVo and HT29 cells with IC50s of 1.4 μM and 1.37 μM, respectively. β-catenin-IN-6 shows cell growth inhibition against several human colorectal cancer lines[1].
β-catenin-IN-6 (compound 9) displays poor bioavailability[1].β-catenin-IN-6 (18.75 mg/kg; ip; once daily for 7 days) decreases tumor volume in mouse model, without affecting body weight[1]. β-catenin-IN-6 (compound 13) (150 mg/kg; ip; once per week) suppresses xenograft tumor growth in a β-catenin/RK3E mouse model[2].
References:
[1]. Dehnhardt CM, et al. Design and synthesis of novel diaminoquinazolines with in vivo efficacy for beta-catenin/T-cell transcriptional factor 4 pathway inhibition. J Med Chem. 2010 Jan 28;53(2):897-910.
[2]. McCoy MA, et al. Biopsical Survey of Small-Molecule β-Catenin Inhibitors: A Cautionary Tale. J Med Chem. 2022 May 26;65(10):7246-7261.