TAK-931 (Simurosertib) is a potent, selective, ATP competitive and orally bioavailable inhibitor of Cdc7 with IC50 of <0.3 nM.
TAK-931 prevents the initiation of DNA replication during mitosis, which causes cell cycle arrest and induces apoptosis.
TAK-931 demonstrates antiproliferative activity with cancer cell lines and tumor growth inhibition (TGI) in murine ectopic xenograft models.
1. Charles Locuson, et al. Abstract 5041: Translational pharmacokinetic-pharmacodynamic xenograft model for TAK-931, a small molecule cell division cycle 7 (CDC7) kinase inhibitor. AACR.
2. Kenichi Iwai, et al. Abstract 3073: Potential predictive biomarkers of clinical responses for a novel CDC7-selective inhibitor TAK-931. AACR.
