Rigosertib
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| Names | |
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| IUPAC name
sodium (E)-2-((2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)amino)acetate
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| Identifiers | |
3D model (JSmol)
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CompTox Dashboard (EPA)
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| Properties | |
| C21H24NNaO8S | |
| Molar mass | 473.47g/mol |
| Boiling point | 756.1±60.0 °C at 760 mmHg |
| Hazards | |
| Flash point | 411.1±32.9 °C |
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 analogue,of which (E)-ON 01910·Na is on a phase III clinical stage anti-cancer agent and its geometrical isomer (Z)-ON 01910·Na is with 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 tumors.
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 .Maybe that's why Rigosertib show little liver damage, or neurotoxicity in mouse xenograft models.
Rigosertib is an non-ATP-competitive inhibitor.It inhibits PLK1 by competing substrate- binding sites with 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.
{{cite journal}}: Check date values in:|date=(help) - ^ "Rigosertib activity data in vitro and in vivo". selleckchemicals. 20 Aug 2014.