Rigosertib
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| Names | |
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| IUPAC name
2‐[(2‐Methoxy‐5‐{[(E)‐2‐(2,4,6‐trimethoxyphenyl)ethenesulfonyl]methyl}phenyl)amino]acetic acid
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| Other names
ON-01910
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| Identifiers | |
3D model (JSmol)
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| ChEMBL | |
| ChemSpider | |
PubChem CID
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CompTox Dashboard (EPA)
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| Properties | |
| C21H25NO8S | |
| Molar mass | 451.49 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Rigosertib (ON-01910 sodium salt, with Estybon as trade name) is a synthetic benzyl styryl sulfone that is in phase III clinical trials as an anti-cancer agent.[citation needed]
Its geometrical isomer (Z)-ON 01910·Na has less cytotoxicity on cancer cells.
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.[2] 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.[3]
References
- ^ "physical and chemical data on chemispider website".
- ^ Nuthalapati S (Sep 2012). "Preclinical pharmacokinetic and pharmacodynamic evaluation of novel anticancer agents, ON01910.Na (Rigosertib, Estybon™) and ON013105, for brain tumor chemotherapy". Pharm Res. 29 (9). doi:10.1007/s11095-012-0780-y. PMID 22678771.
- ^ "Rigosertib activity data in vitro and in vivo". selleckchemicals. 20 Aug 2014.
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