rigosertib
{{Chembox
| Name = Rigosertib
| ImageFile = Rigosertib.svg
| ImageAlt =
| IUPACName = (2-Methoxy-5-
| SystematicName = (2-Methoxy-5-
| OtherNames = ON-01910
|Section1={{Chembox Identifiers
| IUPHAR_ligand = 7833
| CASNo_Ref = {{cascite|correct|CAS}}
| CASNo = 592542-59-1
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 67DOW7F9GL
| PubChem = 6918736
| ChEBI = 145417
| ChemSpiderID = 5293927
| ChEMBL = 1241855
| ChEMBL2 = 2013119
| KEGG = D10154
| SMILES = COC1=C(C=C(C=C1)CS(=O)(=O)/C=C/C2=C(C=C(C=C2OC)OC)OC)NCC(=O)O
| SMILES_Comment = {{cite web|url=http://www.chemspider.com/Chemical-Structure.5293927.html?rid=536d329b-927e-45a8-8495-63b421e6eba5|title=physical and chemical data on chemispider website}}
| StdInChI=1S/C21H25NO8S/c1-27-15-10-19(29-3)16(20(11-15)30-4)7-8-31(25,26)13-14-5-6-18(28-2)17(9-14)22-12-21(23)24/h5-11,22H,12-13H2,1-4H3,(H,23,24)/b8-7+
| StdInChIKey = OWBFCJROIKNMGD-BQYQJAHWSA-N
}}
|Section2={{Chembox Properties
| C=21 | H=25 | N=1 | O=8 | S=1
| Appearance =
| Density =
| MeltingPt =
| BoilingPt =
| Solubility = }}
|Section3={{Chembox Hazards
| MainHazards =
| FlashPt =
| AutoignitionPt = }}
}}
Rigosertib (ON-01910 sodium salt, with Estybon as trade name) is a synthetic benzyl styryl sulfone in development by Onconova Therapeutics.{{Cite web|url=https://finpedia.co/bin/Companies/Onconova%20Therapeutics/|title=Onconova Therapeutics|access-date=2019-04-26}} Rigosertib is in phase III clinical trials for the treatment of chronic myelomonocytic leukemia.{{Cite web|url=https://clinicaltrials.gov/ct2/show/NCT01928537|title = 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|date = 29 June 2020}}
Its geometrical isomer (Z)-ON 01910·Na has less cytotoxicity on cancer cells.
Mechanism
Rigosertib is a microtubule-destabilizing agent.{{cite journal|last1=Jost|first1=M|title=Combined CRISPRi/a-Based Chemical Genetic Screens Reveal that Rigosertib Is a Microtubule-Destabilizing Agent|journal=Molecular Cell|volume=68 |issue=1|pages=210–223.e6|pmid=28985505|pmc=5640507|url=|year=2017|doi=10.1016/j.molcel.2017.09.012}}
References
{{reflist}}
Category:Antineoplastic and immunomodulating drugs
Category:Experimental cancer drugs
{{antineoplastic-drug-stub}}