Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors.
Animals
Antineoplastic Agents
/ pharmacology
Drug Resistance, Neoplasm
Gastrointestinal Stromal Tumors
/ drug therapy
Humans
Mutation
Naphthyridines
Protein Kinase Inhibitors
/ pharmacology
Proto-Oncogene Proteins c-kit
/ genetics
Pyrazoles
Pyrroles
Rats
Receptor, Platelet-Derived Growth Factor alpha
/ genetics
Triazines
Urea
/ analogs & derivatives
Vascular Endothelial Growth Factor A
Journal
Science translational medicine
ISSN: 1946-6242
Titre abrégé: Sci Transl Med
Pays: United States
ID NLM: 101505086
Informations de publication
Date de publication:
29 04 2020
29 04 2020
Historique:
received:
24
08
2019
accepted:
23
03
2020
entrez:
1
5
2020
pubmed:
1
5
2020
medline:
24
6
2021
Statut:
ppublish
Résumé
Gastrointestinal stromal tumor (GIST) is the most common human sarcoma driven by mutations in
Identifiants
pubmed: 32350132
pii: 12/541/eaaz2481
doi: 10.1126/scitranslmed.aaz2481
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Naphthyridines
0
Protein Kinase Inhibitors
0
Pyrazoles
0
Pyrroles
0
Triazines
0
Vascular Endothelial Growth Factor A
0
avapritinib
513P80B4YJ
Urea
8W8T17847W
ripretinib
9XW757O13D
Proto-Oncogene Proteins c-kit
EC 2.7.10.1
Receptor, Platelet-Derived Growth Factor alpha
EC 2.7.10.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Informations de copyright
Copyright © 2020 The Authors, some rights reserved; exclusive licensee American Association for the Advancement of Science. No claim to original U.S. Government Works.