2109805-96-9

BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy[1].

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.

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[1] Ellermann M, et al. Novel Class of Potent and Cellularly Active Inhibitors Devalidates MTH1 as Broad-Spectrum Cancer Target.ACS Chem Biol. 2017 Aug 18;12(8):1986-1992. DOI:10.1021/acschembio.7b00370