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Compound class: Synthetic organic
Comment: CCT196969 is an orally active pan RAF inhibitor that also inhibits SRC family kinases . It was designed to show that the addition of SRC family kinase inhibition alongside RAF inhibition is able to circumvent the paradoxical SRC-mediated re-activation of the RAF-MAP kinase pathway that is observed in tumours with acquired resistance to RAF 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.✖
|CCT196969 has an anti-proliferative effect against patient-derived xenografts from tumours with acquired and intrinsic resistance to the BRAF inhibitor vemurafenib, and against those with acquired resistance to dabrafenib (a BRAFV600E inhibitor) plus trametinib (a MAPK inhibitor) .
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