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TitleRLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations.
Journal, issue, pagesCancer Discov, Vol. 13, Page 2012-2031, Year 2023
Publish dateMay 10, 2023 (structure data deposition date)
AuthorsSubbiah, V. / Sahai, V. / Maglic, D. / Bruderek, K. / Toure, B.B. / Zhao, S. / Valverde, R. / O'Hearn, P.J. / Moustakas, D.T. / Schonherr, H. ...Subbiah, V. / Sahai, V. / Maglic, D. / Bruderek, K. / Toure, B.B. / Zhao, S. / Valverde, R. / O'Hearn, P.J. / Moustakas, D.T. / Schonherr, H. / Gerami-Moayed, N. / Taylor, A.M. / Hudson, B.M. / Houde, D.J. / Pal, D. / Foster, L. / Gunaydin, H. / Ayaz, P. / Sharon, D.A. / Goyal, L. / Schram, A.M. / Kamath, S. / Sherwin, C.A. / Schmidt-Kittler, O. / Jen, K.Y. / Ricard, F. / Wolf, B.B. / Shaw, D.E. / Bergstrom, D.A. / Watters, J. / Casaletto, J.B.
External linksCancer Discov / PubMed:37270847
MethodsX-ray diffraction
Resolution3.79 Å
Structure data

PDB-8stg:
Discovery and clinical validation of RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Method: X-RAY DIFFRACTION / Resolution: 3.79 Å

Chemicals

ChemComp-WCJ:
N-{4-[(5P)-4-amino-5-{3-fluoro-4-[(4-methylpyrimidin-2-yl)oxy]phenyl}-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl}-2-methylpropanamide

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/INHIBITOR / Relay Inhibitor / CYTOSOLIC PROTEIN / TRANSFERASE-INHIBITOR complex

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