Rigosertib

Last updated
Rigosertib
Rigosertib.svg
Names
IUPAC name
(2-Methoxy-5-{{#parsoidfragment:0}}{[(E)-2-(2,4,6-trimethoxyphenyl)ethene-1-sulfonyl]methyl}phenyl)glycine
Systematic IUPAC name
(2-Methoxy-5-{{#parsoidfragment:1}}{[(E)-2-(2,4,6-trimethoxyphenyl)ethene-1-sulfonyl]methyl}anilino)acetate
Other names
ON-01910
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
KEGG
PubChem CID
UNII
  • 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
  • [2] :COC1=C(C=C(C=C1)CS(=O)(=O)/C=C/C2=C(C=C(C=C2OC)OC)OC)NCC(=O)O
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).

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

  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.


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