Rigosertib

Rigosertib

Chemical Structure of Rigosertib
Names
IUPAC name sodium (E)-2-((2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)amino)acetate
Identifiers
CAS Number	1225497-78-8
3D model (JSmol)	Interactive image
CompTox Dashboard (EPA)	DTXSID30207984
SMILES 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	C21H24NNaO8S
Molar mass	473.47g/mol
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 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. 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.