BAY-707

Research use only, not for human use.

BAY-707 is a highly potent, selective and substrate-competitive inhibitor of MTH1 (NUDT1) with IC50 of 2.3 nM.

BAY-707 is a highly potent, selective and substrate-competitive inhibitor of MTH1 (NUDT1) with IC50 of 2.3 nM; demonstrates high selectivity in an in-house kinase panel, and shows an overall favorable physicochemical profile and in vitro pharmacokinetic properties with high metabolic stability; demonstrates a superior cellular target engagement with an EC50 of 7.6 nM compared with TH588, increases the cellular thermal stabilization of MTH1 with no effect on the expression of MTH2, OGG1, and MUTYH; shows a clear lack of in vitro or in vivo anticancer efficacy either in mono- or in combination therapies in vivo.

BAY-707 demonstrates a superior cellular target engagement with an EC50 of 7.6 nM, in agreement with its higher enzymatic potency (IC50=2.3 nM).BAY-707 demonstrates a high cell permeability cell permeability in the Caco-2 assay with a efflux ratio of 288 nm/s.BAY-707 shows an overall favorable physicochemical profile and promising?in vitro?pharmacokinetic properties with high metabolic stability in both human microsomes(0.29L/h/kg,Fmax=78%) and rat hepatocytes (0.54L/h/kg,Fmax=87%) .BAY-707 (0-30 μM; 24 hours) has no antiproliferative effects in HMEC, HeLa and SW-480 cells.

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.BAY-707 (orally adminstation; 50-250 mg/kg; 2 weeks) is well-tolerated in nude mice,after 7-days treatment, body weight loss does not exceed 10% .

BAY 707 | BAY707

Cell Cycle/DNA Damage

DNA Repair Protein

DNA Repair Protein

Cancer

——

2109805-96-9

288.351

C15H20N4O2

>98% (HPLC)

——

O=C(C1=CC2=C(N3[C@@H](C)COCC3)C=CN=C2N1)NCC

(S)-N-ethyl-4-(3-methylmorpholino)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years