Rigosertib (ON-01910 sodium salt, with Estybon as trade name) is a synthetic benzyl styryl sulfone in development by Onconova Therapeutics.[2] Rigosertib is in phase III clinical trials for the treatment of chronic myelomonocytic leukemia.[3]
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| Names | |
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| IUPAC name
(2-Methoxy-5-{[(E)-2-(2,4,6-trimethoxyphenyl)ethene-1-sulfonyl]methyl}phenyl)glycine
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| Systematic IUPAC name
(2-Methoxy-5-{[(E)-2-(2,4,6-trimethoxyphenyl)ethene-1-sulfonyl]methyl}anilino)acetate | |
| Other names
ON-01910
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| Identifiers | |
3D model (JSmol)
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| ChEMBL | |
| ChemSpider | |
| KEGG | |
PubChem CID
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| UNII | |
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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Its geometrical isomer (Z)-ON 01910·Na has less cytotoxicity on cancer cells.
Mechanism
editRigosertib is a microtubule-destabilizing agent.[4]
References
edit- ^ "physical and chemical data on chemispider website".
- ^ "Onconova Therapeutics". Retrieved 2019-04-26.
- ^ "Phase IIIB, Open-label, Multi-Center Study of the Efficacy and Safety of Rigosertib Administered as 72-hour Continuous Intravenous Infusions in Patients with Myelodysplastic Syndrome with Excess Blasts Progressing on or After Azacitidine or Decitabine". 29 June 2020.
- ^ Jost, M (2017). "Combined CRISPRi/a-Based Chemical Genetic Screens Reveal that Rigosertib Is a Microtubule-Destabilizing Agent". Molecular Cell. 68 (1): 210–223.e6. doi:10.1016/j.molcel.2017.09.012. PMC 5640507. PMID 28985505.
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