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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
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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