LGK974 is well-tolerated in Wnt-dependent tissues at an efficacious dose in rats. (A) LGK974 induced tumor regression when dosed at 3 mg/kg per day in a rat MMTV-Wnt1 xenograft tumor model. (B) Intestine, (C) skin/hair follicle, and (D) stomach tissues from rats treated with vehicle control or LGK974 at the dose of 3 mg/kg per day were subjected to H&E staining. (Magnification: intestine, 4×; hair follicle and stomach, 20×. Scale bars: intestine, 500 μM; hair follicle and stomach, 100 μM.)