Rigosertib (sodium)

Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle[1][2]. Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM[3].

Product Specifications

CAS Number

[592542-60-4]

Product Name Alternative

ON-01910 (sodium)

UNSPSC

12352005

Target

Apoptosis; PI3K; Polo-like Kinase (PLK)

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Rigosertib-sodium.html

Purity

99.57

Solubility

DMSO : 150 mg/mL (ultrasonic) |H2O : ≥ 52 mg/mL

Smiles

COC1=CC=C(C=C1NCC(O[Na])=O)CS(/C=C/C2=C(C=C(C=C2OC)OC)OC)(=O)=O

Molecular Formula

C21H24NNaO8S

Molecular Weight

473.47

References & Citations

[1]Xu F, et al. Rigosertib as a selective anti-tumor agent can ameliorate multiple dysregulated signalingtransduction pathways in high-grade myelodysplastic syndrome. Sci Rep. 2014 Dec 4;4:7310.|[2]Hyoda T, et al. Rigosertib induces cell death of a myelodysplastic syndrome-derived cell line by DNA damage-induced G2/M arrest. Cancer Sci. 2015 Mar;106 (3) :287-93.|[3]Gumireddy K, et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell. 2005 Mar;7 (3) :275-86.|[4]Reddy MV, et al. Discovery of a clinical stage multi-kinase inhibitor sodium (E) -2-{2-methoxy-5-[ (2',4',6'-trimethoxystyrylsulfonyl) methyl]phenylamino}acetate (ON 01910.Na) : synthesis, structure-activity relationship, and biological activity. J Med Chem.|[5]Chapman CM, et al. ON 01910.Na is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Clin Cancer Res. 2012 Apr 1;18 (7) :1979-91