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Structure paper

TitleA novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells withFLT3mutations.
Journal, issue, pagesBlood, Vol. 131, Page 426-438, Year 2018
Publish dateJan 19, 2017 (structure data deposition date)
AuthorsYamaura, T. / Nakatani, T. / Uda, K. / Ogura, H. / Shin, W. / Kurokawa, N. / Saito, K. / Fujikawa, N. / Date, T. / Takasaki, M. ...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.
External linksBlood / PubMed:29187377
MethodsX-ray diffraction
Resolution2.401 Å
Structure data

PDB-5x02:
Crystal structure of the FLT3 kinase domain bound to the inhibitor FF-10101
Method: X-RAY DIFFRACTION / Resolution: 2.401 Å

Chemicals

ChemComp-F6M:
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

ChemComp-SO4:
SULFATE ION

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INIHIBITOR / tyrosine kinase / transferase / irreversible inhibitor complex / kinase catalytic domain / TRANSFERASE-TRANSFERASE INIHIBITOR complex

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