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Synonyms: compound 18 [PMID: 31250638]
Compound class: Synthetic organic
Comment: CHMFL-KIT-64 is a potent and orally available inhibitor of wild-type c-KIT and a range of known c-KIT resistance mutants . It has demonstrated anti-tumour efficacy in vitro, in mouse xenograft models, and against imatinib-resistant patient tumour cells expressing wild-type c-KIT. It has been proposed as a potential clinical lead for gastrointestinal stromal tumour (GIST) therapy as the majority (80-85%) of GISTs harbour c-KIT activation mutations. Other c-KIT mutations confer primary or secondary (acquired) resistance to imatinib which is the first line drug used to combat GISTs. CHMFL-KIT-64 was designed to target mutations that are refractory to currently approved therapeutics including imatinib, sunitinib and regorafenib. It can potently inhibit the T670I ATP binding pocket (gatekeeper) mutant that is resistant to many other c-KIT inhibitors.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Wu Y, Wang B, Wang J, Qi S, Zou F, Qi Z, Liu F, Liu Q, Chen C, Hu C et al.. (2019)
Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors.
J Med Chem, 62 (13): 6083-6101. [PMID:31250638]