Chemical Structure : ART5537
CAS No.:
ART5537
(ART-5537)
Catalog No.: PC-26135Not For Human Use, Lab Use Only.
ART5537 (ART-5537) is highly potent and selective inhibitor of Exonuclease 1 (EXO1) with IC50 of 3.4 nM, inhibits homologous recombination (HR) with EC50 of 7.2 nM in HR reporter assays.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
ART5537 (ART-5537) is highly potent and selective inhibitor of Exonuclease 1 (EXO1) with IC50 of 3.4 nM, inhibits homologous recombination (HR) with EC50 of 7.2 nM in HR reporter assays.
ART5537 direcly binds to EXO1 with SPR KD of 6.8 nM.
ART5537 displays ≥200-fold selectivity over a panel of the wider nuclease superfamily, including DNA2, MRE11, MUS81, SNM1A etc.
ART5537 displays unambiguous dose-dependent cellular target engagement with an EC50 of 55 nM.
ART5537 kills MDA-MB-436 and HCC1937 (BRCA1 null), SUM149PT (BRCA1 Δ11q hypomorph), and HCC38 (BRCA1 promoter methylated) breast cancer cells in the low micromolar range, exhibits strong sensitization to ionizing radiation (IR) in HCT116 cells.
Physicochemical Properties
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M.Wt
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447.88
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Formula
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C23H18ClN5O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-1-(4-Chloro-2,7-naphthyridin-1-yl)-5-hydroxy-3-(1-phenylethyl)-2,3-dihydro-1H-pyrido[2,1-f][1,2,4]triazine-4,6-dione
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References
1. Sam E Mann, et al. J Med Chem. 2025 Dec 25;68(24):26432-26447.
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