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Synonyms: GCD-516 | GCD516 | MGCD516
Compound class: Synthetic organic
Comment: Sitravatinib (MGCD516) is an inhibitor of multiple receptor tyrosine kinases (RTKs) that was developed as an antineoplatic agent . It targets several RTKs (e.g. c-Met, PDGFR, c-Kit and IGF1-R) whose overexpression has been shown to drive sarcoma cell growth
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.✖
|Sitravatinib is reported to produce superior antiproliferative efficacy than imatinib and crizotinib in vitro and in vivo .
A selection of the inhibitory IC50s reported in  (Table 1) are included in our table below. In some cases we have restricted our selection to the most potently inhibited isoform from each subfamily of RTKs that were tested.
|Selectivity at catalytic receptors|
|Key to terms and symbols||Click column headers to sort|