Synonyms: MP 470 | MP-470 | MP470
Compound class:
Synthetic organic
Comment: Amuvatinib is an orally bioavailable, multitargeted receptor tyrosine kinase inhibitor. Some bioactivity data may be associated with the hydrochloride salt (PubChem CID 67254077).
Ligand Activity Visualisation ChartsThese 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. ✖ |
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No information available. |
Summary of Clinical Use |
A Phase 2 clinical trial for small cell lung cancer (in combination with platinum-etoposide chemotherapy) was registered with ClinicalTrials.gov, but details have not been updated since 2012. |
Mechanism Of Action and Pharmacodynamic Effects |
Amuvatinib binds to and inhibits the activity of mutant forms of the stem cell factor receptor (c-Kit, mutant forms of which are often associated with tumor chemoresistance [2]), AXL [2] and other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3 and PDGFRα, which are frequently dysregulated in variety of tumours. In addition, this compound suppresses the induction of the DNA repair protein RAD51 recombinase (HGNC ID 9817), thereby potentiating the activities of DNA damage-inducing agents [3-4]. |