- Guide to PHARMACOLOGY
Synonyms: Chir 258 | CHIR-258 | TKI 258 | TKI-258
Compound class: Synthetic organic
Comment: Dovitinib is a multi-targeted receptor tyrosine kinase (RTK) inhibitor, with modest selectivity for Class III RTKs (IC50s 1-2nM), with IC50s for Class IV and V RTKs in the 8-13nM range. Please note that ChEMBL represents this compound as a tautomer of our structure.
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.✖
|No information available.
|Summary of Clinical Use
|Dovitinib progressed to Phase 3 evaluation in patients with advanced solid tumours. Click here to link to ClinicalTrials.gov's currently registered drug trials involving this compound. Most of these studies are marked as 'terminated' (a few due to drug toxicity concerns), 'withdrawn' or 'completed'.
|Mechanism Of Action and Pharmacodynamic Effects
|This compound inhibits key receptor tyrosine kinases that are implicated in tumor vasculature formation and maintenance, and which underlie tumor progression and metastasis.