7ZW8

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

Summary for 7ZW8

Entry DOI	10.2210/pdb7zw8/pdb
Descriptor	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)
Functional Keywords	tyrosine-protein kinase, ckit, transferase
Biological source	Homo sapiens (human)
Total number of polymer chains	1
Total formula weight	37686.57
Authors	Graedler, U.,Lammens, A. (deposition date: 2022-05-19, release date: 2023-02-22, Last modification date: 2024-02-07)
Primary citation	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 Cited by PubMed: 36728508 DOI: 10.1021/acs.jmedchem.2c00851 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.119 Å)

Structure validation