7ZW8

Identification of M4205 a highly selective inhibitor of cKIT mutations for unresectable metastatic or recurrent GIST

7ZW8 の概要

• エントリーDOI: 10.2210/pdb7zw8/pdb
• 分子名称: Mast/stem cell growth factor receptor Kit, ~{N}-[[4-(1-methylpyrazol-4-yl)phenyl]methyl]-6-[7-(3-pyrrolidin-1-ylpropoxy)imidazo[1,2-a]pyridin-3-yl]pyrimidin-4-amine (3 entities in total)
• 機能のキーワード: tyrosine-protein kinase, ckit, transferase
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 37686.57

構造登録者

Graedler, U.,Lammens, A. (登録日: 2022-05-19, 公開日: 2023-02-22, 最終更新日: 2024-02-07)

• 主引用文献: Blum, A.,Dorsch, D.,Linde, N.,Brandstetter, S.,Buchstaller, H.P.,Busch, M.,Glaser, N.,Gradler, U.,Ruff, A.,Petersson, C.,Schieferstein, H.,Sherbetjian, E.,Esdar, C.; Identification of M4205─A Highly Selective Inhibitor of KIT Mutations for Treatment of Unresectable Metastatic or Recurrent Gastrointestinal Stromal Tumors.; J.Med.Chem., 66:2386-2395, 2023; PubMed: 36728508; DOI: 10.1021/acs.jmedchem.2c00851

実験手法

X-RAY DIFFRACTION (2.119 Å)