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BAY-707

Catalog No. T14509 CAS 2109805-96-9

BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1].

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BAY-707, CAS 2109805-96-9

Pack Size	Availability	Price/USD	Quantity
5 mg	35 days	$ 340.00
25 mg	35 days	$ 1,430.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1].
Targets&IC50	MTH1/NUDT1:2.3 nM
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] and it also demonstrates a high cell permeability cell permeability in the Caco-2 assay with a efflux ratio of 288 nm/s[1]. BAY-707 (0-30 μM; 24 hours) has no antiproliferative effects in HMEC, HeLa and SW-480 cells[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].
In vivo	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] and it also exhibits superior biochemical potency, cellular target engagement, and a pharmacokinetic profile to other MTH1 tool compounds. However, Bay-077 exerts no anticancer efficacy either in mono- or in combination therapies in CT26 and NCI-H460 mice model[1].

Molecular Weight	288.34
Formula	C15H20N4O2
CAS No.	2109805-96-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BAY-707 2109805-96-9 Others BAY707 BAY 707 inhibitor inhibit

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