Formula C21H25NO8S | ChemSpider ID 5293927 | |
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Bone marrow blast response to overall survival higher risk mds rigosertib after failure of hmas
Rigosertib (ON-01910 sodium salt, with Estybon as trade name) is a synthetic benzyl styryl sulfone in development by Onconova Therapeutics. Riosertib is in phase III clinical trials for the treatment of chronic myelomonocytic leukemia.
Contents
- Bone marrow blast response to overall survival higher risk mds rigosertib after failure of hmas
- Phase i ii study combination rigosertib and azacitidine in patients with mds or aml
- Mechanism
- References
Its geometrical isomer (Z)-ON 01910·Na has less cytotoxicity on cancer cells.
Phase i ii study combination rigosertib and azacitidine in patients with mds or aml
Mechanism
Rigosertib is a small molecule inhibitor, which simultaneously inhibits PI3K and PLK signaling pathways.The over-expression of these two pathways may lead occurrence and development of many kinds of tumors. Thus rigosertib performs potential antineoplastic activity in multiple tumor types.
Rigosertib can convert the gene express profilings, cause mitotic cell-cycle G2 arrest of tumor cells, leading their apoptosis. And what it causes in normal cells is a reversible cell arrest at the G1 and G2 stage without apoptosis. Rigosertib shows little liver damage or neurotoxicity in mouse xenograft models.
Rigosertib is an non-ATP-competitive inhibitor. It inhibits PLK1 by competing at substrate-binding sites with an IC50 of 9 nM.