BAY707)
BAY-707
CAS: 2109805-96-9
Molecular Formula: C15H20N4O2
BAY707) - Names and Identifiers
BAY707) - Physico-chemical Properties
| Molecular Formula | C15H20N4O2 |
| Molar Mass | 288.34 |
| Density | 1.225±0.06 g/cm3(Predicted) |
| pKa | 14.36±0.40(Predicted) |
| Storage Condition | 2-8°C，密封，干燥 |
| In vitro study | BAY-707 demonstrates a superior cellular target engagement with an EC 50 of 7.6 nM, in agreement with its higher enzymatic potency (IC 50 =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 promisingin vitropharmacokinetic properties with high metabolic stability in both human microsomes(0.29L/h/kg,F max =78%) and rat hepatocytes (0.54L/h/kg,F max =87%) . BAY-707 (0-30 μM; 24 hours) has no antiproliferative effects in HMEC, HeLa and SW-480 cells. |
| In vivo study | 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% . |
BAY707) - Reference Information
| biological activity | BAY-707 is a substrate competitive, highly selective inhibitor of MTH1 (nutt1), the IC50 value was 2.3 nM. BAY-707 has a good pharmacokinetic profile compared to other MTH1 compounds and is well tolerated in mice, but the experiment clearly lacks anti-cancer efficacy in vitro or in vivo. |
| Target | IC50:2.3 nM (MTH1/NUDT1) |
Last Update：2024-04-09 21:22:08
