9TFM

KIT kinase domain in complex with a 7-methoxyquinazolin-6-ol-based compound (45)

Summary for 9TFM

Entry DOI	10.2210/pdb9tfm/pdb
Descriptor	Mast/stem cell growth factor receptor Kit, 4-[4-[5-[(1~{S})-1-azanyl-1-(4-fluorophenyl)ethyl]pyrimidin-2-yl]piperazin-1-yl]-7-methoxy-quinazolin-6-ol (3 entities in total)
Functional Keywords	kit protein kinase, inhibitor, tyrosine kinase, transmembrane receptor, stem cell factor, scf, stem cell factor receptor, gist, gastrointestinal stromal tumors, p10721, transferase
Biological source	Homo sapiens (human) More
Total number of polymer chains	2
Total formula weight	75339.90
Authors	Scrima, A.,Mueller, M.P.,Rauh, D. (deposition date: 2025-11-27, release date: 2026-07-15)
Primary citation	Schulz, T.,Beerbaum, M.,Scrima, A.,Jantzen, H.,Teuber, A.,Muehlenberg, T.,Garcia-Fossa, F.,Weisner, J.,Mueller, M.P.,Sievers, S.,Bauer, S.,Rauh, D. Structure-based Scaffold Hopping Reveals Strategies to Overcome Oncogenic KIT and PDGFRA Mutation-Driven Drug-Resistance in GIST To Be Published,
Experimental method	X-RAY DIFFRACTION (2.1 Å)

Structure validation