Rigosertib

Rigosertib
Names
	Preferred IUPAC name (2-Methoxy-5-{[(1E)-2-(2,4,6-trimethoxyphenyl)ethene-1-sulfonyl]methyl}anilino)acetate
	Other names ON-01910
Identifiers
CAS Number	592542-59-1 ;
3D model (JSmol)	[1]: Interactive image;
ChEBI	CHEBI:145417;
ChEMBL	ChEMBL1241855; ChEMBL2013119;
ChemSpider	5293927;
IUPHAR/BPS	7833;
KEGG	D10154;
PubChem CID	6918736;
UNII	67DOW7F9GL ;
CompTox Dashboard (EPA)	DTXSID30207984 ;
	InChI InChI=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+ Key: OWBFCJROIKNMGD-BQYQJAHWSA-N;
	SMILES [2]: COC1=C(C=C(C=C1)CS(=O)(=O)/C=C/C2=C(C=C(C=C2OC)OC)OC)NCC(=O)O;
Properties
Chemical formula	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). Infobox references

Rigosertib (ON-01910 sodium salt, with Estybon as trade name) is a synthetic benzyl styryl sulfone in development by Onconova Therapeutics.[3] Rigosertib is in phase III clinical trials for the treatment of chronic myelomonocytic leukemia.[4]

Its geometrical isomer (Z)-ON 01910·Na has less cytotoxicity on cancer cells.

Mechanism

Rigosertib is a microtubule-destabilizing agent.[5]

References

"physical and chemical data on chemispider website".
"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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[1] "physical and chemical data on chemispider website".

[2] "physical and chemical data on chemispider website".

[3] "Onconova Therapeutics". Retrieved 2019-04-26.

[4] "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.

[5] 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.