Synonyms: Estybon® (proposed trade name) | ON-01910 | ON01910.Na
Compound class:
Synthetic organic
Comment: Rigosertib is a dual kinase inhibitor, affecting the phosphoinositide 3-kinase (PI3K) and polo-like kinase 1 (PLK1) pathways. Note that the inhibitory action on PLK1 has been disputed [2]. It is a non-ATP-competitive inhibitor, meaning it inhibits substrate binding to the enzyme.
Note that some bioactivity data may be associated with the sodium salt, PubChem CID 23696523. 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 |
Rigosertib has been granted orphan designation by the EMA and US FDA for myelodysplastic syndromes (MDS). Rigosertib is in Phase 3 clinical trials as an anti-neoplastic. Click here to access ClinicalTrials.gov's registered Phase 3 trials assessing rigosertib. |
Mechanism Of Action and Pharmacodynamic Effects |
Rigostertib causes mitotic cell-cycle arrest of tumor cells which leads to their apoptosis [1]. |