BAY-707 is a substrate-competitive, highly selective inhibitor of MTH1(NUDT1) with IC50 of 2.3 nM. It has a favorable pharmacokinetic profile compared to other MTH1 compounds and is well tolerated in mice, but the experiments clearly lack in vitro or in vivo anticancer efficacy.
Bay-077 (orally adminstation; 50-250 mg/kg; 2 weeks) exhibits superior biochemical potency, cellular target engagement, and a pharmacokinetic profile to other MTH1 tool compounds, But Bay-077 exerts no anticancer efficacy either in mono- or in combination therapies in CT26 and NCI-H460 mice model.