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AZD4625 is a Potent and Selective Inhibitor of KRASG12C.
Chakraborty, Atanu; Hanson, Lyndsey; Robinson, David; Lewis, Hilary; Bickerton, Sue; Davies, Michael; Polanski, Radoslaw; Whiteley, Rebecca; Koers, Alex; Atkinson, James; Baker, Tamara; Del Barco Barrantes, Ivan; Ciotta, Giovanni; Kettle, Jason G; Magiera, Lukasz; Martins, Carla P; Peter, Alison; Wigmore, Eleanor; Underwood, Zoe; Cosulich, Sabina; Niedbala, Michael; Ross, Sarah.
Afiliación
  • Chakraborty A; AstraZeneca, Cambridge, United Kingdom.
  • Hanson L; AstraZeneca, Cambridge, United Kingdom.
  • Robinson D; AstraZeneca, Cambridge, United Kingdom.
  • Lewis H; AstraZeneca, Cambridge, United Kingdom.
  • Bickerton S; AstraZeneca, Cambridge, United Kingdom.
  • Davies M; AstraZeneca, Cambridge, United Kingdom.
  • Polanski R; AstraZeneca, Cambridge, United Kingdom.
  • Whiteley R; AstraZeneca, Cambridge, United Kingdom.
  • Koers A; AstraZeneca, Cambridge, United Kingdom.
  • Atkinson J; AstraZeneca, Cambridge, United Kingdom.
  • Baker T; AstraZeneca, Cambridge, United Kingdom.
  • Del Barco Barrantes I; AstraZeneca, Cambridge, United Kingdom.
  • Ciotta G; AstraZeneca, Cambridge, United Kingdom.
  • Kettle JG; AstraZeneca, Cambridge, United Kingdom.
  • Magiera L; AstraZeneca, Cambridge, United Kingdom.
  • Martins CP; AstraZeneca, Cambridge, United Kingdom.
  • Peter A; AstraZeneca, Cambridge, United Kingdom.
  • Wigmore E; AstraZeneca, Cambridge, United Kingdom.
  • Underwood Z; AstraZeneca, Cambridge, United Kingdom.
  • Cosulich S; AstraZeneca, Cambridge, United Kingdom.
  • Niedbala M; AstraZeneca, Waltham, Massachusetts.
  • Ross S; AstraZeneca, Cambridge, United Kingdom.
Mol Cancer Ther ; 21(10): 1535-1546, 2022 10 07.
Article en En | MEDLINE | ID: mdl-35930755
AZD4625 is a potent, selective, and orally bioavailable inhibitor of oncogenic KRASG12C as demonstrated in cellular assays and in vivo in preclinical cell line-derived and patient-derived xenograft models. In vitro and cellular assays have shown selective binding and inhibition of the KRASG12C mutant isoform, which carries a glycine to cysteine mutation at residue 12, with no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. The pharmacology of AZD4625 shows that it has the potential to provide therapeutic benefit to patients with KRASG12C mutant cancer as either a monotherapy treatment or in combination with other targeted drug agents.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Cisteína / Antineoplásicos Límite: Humans Idioma: En Revista: Mol Cancer Ther Asunto de la revista: ANTINEOPLASICOS Año: 2022 Tipo del documento: Article País de afiliación: Reino Unido Pais de publicación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Cisteína / Antineoplásicos Límite: Humans Idioma: En Revista: Mol Cancer Ther Asunto de la revista: ANTINEOPLASICOS Año: 2022 Tipo del documento: Article País de afiliación: Reino Unido Pais de publicación: Estados Unidos