Rigosertib

CAT: 0804-HY-12037A-01Size: 5 mgDry Ice: NoHazardous: No

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CAT#:0804-HY-12037A-01Size:5 mg

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Description

Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle[1][2]. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM[3].

CAS Number

592542-59-1

Product Name Alternative

ON-01910

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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.html

Purity

99.01

Solubility

DMSO : 75 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C21H25NO8S

Molecular Weight

451.49

Precautions

H302, H315, H319, H335

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. 2011 Sep 22;54 (18) :6254-76.|[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

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

PLK1; PLK2

Citation 01

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Rigosertib

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