9DF3

EGFR Exon20 insertion mutant SVD bound with (S)-3-((3-chloro-2-methoxyphenyl)amino)-2-(3-((tetrahydrofuran-2-yl)methoxy)pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one

This is a non-PDB format compatible entry.

Summary for 9DF3

• Entry DOI: 10.2210/pdb9df3/pdb
• Descriptor: Epidermal growth factor receptor, 3-[(3-chloranyl-2-methoxy-phenyl)amino]-2-[3-[[(2S)-oxolan-2-yl]methoxy]pyridin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one, 1,2-ETHANEDIOL, ... (5 entities in total)
• Functional Keywords: kinase, inhibitor, oncoprotein, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 39010.30

Authors

Hilbert, B.J.,Brooijmans, N.,Pagliarini, R.A.,Milgram, B.C. (deposition date: 2024-08-29, release date: 2025-05-14)

• Primary citation: Pagliarini, R.A.,Henderson, J.A.,Borrelli, D.R.,Brooijmans, N.,Hilbert, B.J.,Huff, M.R.,Ito, T.,Kryukov, G.,Ladd, B.,Martin, B.,Milgram, B.C.,Motiwala, H.,OHearn, E.,Wang, W.,Hata, A.,Bellier, J.,Kuzmic, P.,Guzman-Perez, A.,Jackson, E.L.,Stuart, D.; STX-721, a covalent EGFR/HER2 exon 20 inhibitor, takes advantage of exon 20 mutant dynamic protein states and achieves unique mutant-selectivity across human cancer models; To Be Published,

Experimental method

X-RAY DIFFRACTION (1.68 Å)