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Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
Boezio, Alessandro A; Copeland, Katrina W; Rex, Karen; K Albrecht, Brian; Bauer, David; Bellon, Steven F; Boezio, Christiane; Broome, Martin A; Choquette, Deborah; Coxon, Angela; Dussault, Isabelle; Hirai, Satoko; Lewis, Richard; Lin, Min-Hwa Jasmine; Lohman, Julia; Liu, Jingzhou; Peterson, Emily A; Potashman, Michele; Shimanovich, Roman; Teffera, Yohannes; Whittington, Douglas A; Vaida, Karina R; Harmange, Jean-Christophe.
Afiliación
  • Boezio AA; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Copeland KW; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Rex K; Amgen Incorporated , One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • K Albrecht B; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Bauer D; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Bellon SF; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Boezio C; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Broome MA; Amgen Incorporated , One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Choquette D; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Coxon A; Amgen Incorporated , One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Dussault I; Amgen Incorporated , One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Hirai S; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Lewis R; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Lin MH; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Lohman J; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Liu J; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Peterson EA; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Potashman M; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Shimanovich R; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Teffera Y; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Whittington DA; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Vaida KR; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Harmange JC; Amgen Incorporated , 360 Binney Street, Cambridge, Massachusetts 02142, United States.
J Med Chem ; 59(6): 2328-42, 2016 Mar 24.
Article en En | MEDLINE | ID: mdl-26812066
ABSTRACT
Deregulation of the receptor tyrosine kinase mesenchymal epithelial transition factor (MET) has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of compound 23 (AMG 337), which demonstrates nanomolar inhibition of MET kinase activity, desirable preclinical pharmacokinetics, significant inhibition of MET phosphorylation in mice, and robust tumor growth inhibition in a MET-dependent mouse efficacy model.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piridonas / Triazoles / Proteínas Proto-Oncogénicas c-met / Antineoplásicos Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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PubMed Links
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piridonas / Triazoles / Proteínas Proto-Oncogénicas c-met / Antineoplásicos Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Estados Unidos