Description: Crenigacestat (LY3039478) is an orally bioavailable Notch inhibitor with an IC50 of ~1 nM in most tumor cell lines tested. It effectively inhibits mutant Notch receptor activity and, in a xenograft tumor model, inhibits the expression of Notch-regulated genes and N1ICD cleavage in the tumor...

Crenigacestat is an orally bioavailable Notch inhibitor. It induces cell cycle arrest at the G0/G1 phase and decreases expression of the oncogenes MYC and CCNA1 in Caki human renal cancer cells. Crenigacestat (8 mg/kg per day) reduces tumor growth and increases survival in a 769-P mouse xenograft model.Formal Name:...