Discovery of 6‑[(3S,4S)‑4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor

Src homology 2 (SH2) domain-containing phosphatase 2 (SHP2) plays a role in receptor tyrosine kinase (RTK), neurofibromin-1 (NF-1), and Kirsten rat sarcoma virus (KRAS) mutant-driven cancers, as well as in RTK-mediated resistance, making the identification of small-molecule therapeutics that interfe...

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Veröffentlicht in:	Journal of medicinal chemistry 2021-10, Vol.64 (20), p.15141-15169
Hauptverfasser:	Czako, Barbara, Sun, Yuting, McAfoos, Timothy, Cross, Jason B, Leonard, Paul G, Burke, Jason P, Carroll, Christopher L, Feng, Ningping, Harris, Angela L, Jiang, Yongying, Kang, Zhijun, Kovacs, Jeffrey J, Mandal, Pijus, Meyers, Brooke A, Mseeh, Faika, Parker, Connor A, Yu, Simon S, Williams, Christopher C, Wu, Qi, Di Francesco, Maria Emilia, Draetta, Giulio, Heffernan, Timothy, Marszalek, Joseph. R, Kohl, Nancy E, Jones, Philip
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antineoplastic Agents - administration & dosage Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Cell Line, Tumor Cell Proliferation - drug effects Dose-Response Relationship, Drug Drug Discovery Drug Screening Assays, Antitumor Enzyme Inhibitors - administration & dosage Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Mice Molecular Structure Neoplasms, Experimental - drug therapy Neoplasms, Experimental - metabolism Neoplasms, Experimental - pathology Protein Tyrosine Phosphatase, Non-Receptor Type 11 - antagonists & inhibitors Protein Tyrosine Phosphatase, Non-Receptor Type 11 - metabolism Structure-Activity Relationship
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