5X02

Crystal structure of the FLT3 kinase domain bound to the inhibitor FF-10101

Summary for 5X02

• Entry DOI: 10.2210/pdb5x02/pdb
• Descriptor: Receptor-type tyrosine-protein kinase FLT3, N-[(2S)-1-[5-[2-[(4-cyanophenyl)amino]-4-(propylamino)pyrimidin-5-yl]pent-4-ynylamino]-1-oxidanylidene-propan-2-yl]-4-(dimethylamino)-N-methyl-but-2-enamide, SULFATE ION, ... (4 entities in total)
• Functional Keywords: tyrosine kinase, transferase, irreversible inhibitor complex, kinase catalytic domain, transferase-transferase inihibitor complex, transferase/transferase inihibitor
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 1
• Total formula weight: 40829.40

Authors

Fujikawa, N.,Hirano, D.,Takasaki, M.,Terada, D.,Hagiwara, S.,Park, S.-Y.,Sugiyama, K. (deposition date: 2017-01-19, release date: 2018-01-24, Last modification date: 2023-11-22)

• Primary citation: Yamaura, T.,Nakatani, T.,Uda, K.,Ogura, H.,Shin, W.,Kurokawa, N.,Saito, K.,Fujikawa, N.,Date, T.,Takasaki, M.,Terada, D.,Hirai, A.,Akashi, A.,Chen, F.,Adachi, Y.,Ishikawa, Y.,Hayakawa, F.,Hagiwara, S.,Naoe, T.,Kiyoi, H.; A novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells withFLT3mutations.; Blood, 131:426-438, 2018; PubMed: 29187377; DOI: 10.1182/blood-2017-05-786657

Experimental method

X-RAY DIFFRACTION (2.401 Å)