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TitlePf-06463922 is a Potent and Selective Next-Generation Ros1/Alk Inhibitor Capable of Blocking Crizotinib-Resistant Ros1 Mutations.
Journal, issue, pagesProc. Natl. Acad. Sci. USA, Vol. 112, Page 3493-, Year 2015
Publish dateAug 25, 2014 (structure data deposition date)
AuthorsZou, H.Y. / Li, Q. / Engstrom, L.D. / West, M. / Appleman, V. / Wong, K.A. / Mctigue, M. / Deng, Y. / Liu, W. / Brooun, A. ...Zou, H.Y. / Li, Q. / Engstrom, L.D. / West, M. / Appleman, V. / Wong, K.A. / Mctigue, M. / Deng, Y. / Liu, W. / Brooun, A. / Timofeevski, S. / Mcdonnell, S.R.P. / Jiang, P. / Falk, M.D. / Lappin, P.B. / Affolter, T. / Nichols, T. / Hu, W. / Lam, J. / Johnson, T.W. / Smeal, T. / Charest, A. / Fantin, V.R.
External linksProc. Natl. Acad. Sci. USA / PubMed:25733882
MethodsX-ray diffraction
Resolution2.4 Å
Structure data

PDB-4uxl:
Structure of Human ROS1 Kinase Domain in Complex with PF-06463922
Method: X-RAY DIFFRACTION / Resolution: 2.4 Å

Chemicals

ChemComp-5P8:
(10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile / medication, anticancer, inhibitor*YM

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / INHIBITOR / ROS

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