Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.

doi:10.1021/acs.jmedchem.8b00938

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Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.

Journal of medicinal chemistry - 11 Oct 2018

Kettle Jason G, Anjum Rana, Barry Evan, Bhavsar Deepa, Brown Crystal, Boyd Scott, Campbell Andrew, Goldberg Kristin, Grondine Michael, Guichard Sylvie, Hardy Christopher J, Hunt Tom, Jones Rhys D O, Li Xiuwei, Moleva Olga, Ogg Derek, Overman Ross C, Packer Martin J, Pearson Stuart, Schimpl Marianne, Shao Wenlin, Smith Aaron, Smith James M, Stead Darren, Stokes Steve, Tucker Michael, Ye Yang

Abstract excerpt

While the treatment of gastrointestinal stromal tumors (GISTs) has been revolutionized by the application of targeted tyrosine kinase inhibitors capable of inhibiting KIT-driven proliferation, diverse mutations to this kinase drive resistance to established therapies. Here we describe the identification of potent pan-KIT mutant kinase inhibitors that can be dosed without being limited by the tolerability issues...

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PMID: 30204441
DOI: 10.1021/acs.jmedchem.8b00938

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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