Discovery of novel heteroaryl alkynes for highly potent KIT^(D816V) cells inhibition to treat gastrointestinal stromal tumors

摘要

To the Editor:Gastrointestinal stromal tumors(GIST)is the most popular mesenchymal tumor in the gastrointestinal tract with approximately 80%of GIST harboring gain-of-function mutations at either the extracellular region(exon 9)or the juxtamembrane domain(JMD,exon 11)of KIT,resulting in uncontrolled proliferation and resistance to apotosis1.