1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. BAY-707

BAY-707 

Cat. No.: HY-112081
Handling Instructions

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.

For research use only. We do not sell to patients.

BAY-707 Chemical Structure

BAY-707 Chemical Structure

CAS No. : 2109805-96-9

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Description

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].

IC50 & Target

IC50:2.3 nM (MTH1/NUDT1)[1]

In Vitro

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)[1].
BAY-707 demonstrates a high cell permeability cell permeability in the Caco-2 assay with a efflux ratio of 288 nm/s[1].
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%) [1].
BAY-707 (0-30 μM; 24 hours) has no antiproliferative effects in HMEC, HeLa and SW-480 cells[1].

In Vivo

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[1].
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% [1].

Molecular Weight

288.34

Formula

C₁₅H₂₀N₄O₂

CAS No.

2109805-96-9

SMILES

O=C(NCC)C(N1)=CC2=C1N=CC=C2N3CCOC[[email protected]@H]3C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

BAY-707BAY707BAY 707DNA/RNA SynthesisInhibitorinhibitorinhibit

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HY-112081
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