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8STG

Discovery and clinical validation of RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations

Entity
Entity IDChain IDDescriptionTypeChain lengthFormula weightNumber of moleculesDB Name (Accession)Biological sourceDescriptive keywords
1A, B
(A, B)
Fibroblast growth factor receptor 2polymer31736284.82UniProt (P21802)
Pfam (PF07714)
Homo sapiens (human)FGFR-2,K-sam,KGFR,Keratinocyte growth factor receptor
2C, D
(A, B)
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-methylpropanamidenon-polymer511.62Chemie (WCJ)
Sequence modifications
A, B: 458 - 769 (UniProt: P21802)
PDBExternal DatabaseDetails
Ser 453-expression tag
His 454-expression tag
Met 455-expression tag
Gly 456-expression tag
Ser 457-expression tag
Sequence viewer
Contents of the asymmetric unit
PolymersNumber of chains2
Total formula weight72569.6
Non-Polymers*Number of molecules2
Total formula weight1023.1
All*Total formula weight73592.7
*Water molecules are not included.

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PDB entries from 2025-06-18

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