Chemical Name: 7-Fluoro-6-[6-(methoxymethyl)-3-pyridinyl]-4-[[(1S)-1-(1-methyl-1H-pyrazol-3-yl)ethyl]amino]-3-quinolinecarboxamide
Biological ActivityPotent and selective ATM kinase inhibitor (IC50 = 0.6 nM in an enzyme inhibition assay). Exhibits > 600-fold selectivity for ATM over other kinases. Inhibits ATM kinase in an in vitro cellular assay (IC50 = 0.33 μM). Potentiates the antitumor effects of the topoisomerase 1 inhibitor irinotecan (CPT 11, Cat. No. 2688) in tumor bearing, immunocompromised mice. Orally bioavailable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of novel 3-quinoline carboxamides as potent, selective and orally bioavailable inhibitors of ataxia telangiectasia mutated (ATM) kinase.
Degorce et al.
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