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Rigosertib

Catalog No. T16750   CAS 592542-59-1
Synonyms: PI3K, Polo-like Kinase (PLK), Rigosertib, Phosphoinositide 3-kinase, Apoptosis, ON 01910, Inhibitor, ON-01910, inhibit, ON01910

Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition of the PI3 kinase/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in the cell cycle.

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Rigosertib, CAS 592542-59-1
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Purity: 98%
Biological Description
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Description Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition of the PI3 kinase/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in the cell cycle.
Targets&IC50 Fyn:182 nM, CDK1:260 nM, PDGFR:18 nM, Flt1:42 nM, PLK1:9 nM, PLK2:260 nM, Bcr-Abl:32 nM, Src:155 nM
In vitro Rigosertib is a non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib displays cell killing activity against 94 different tumor cell lines (IC50: 50-250 nM), including BT27, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, SW480, and KB cells. Rigosertib also shows inhibition of PLK2, PDGFR, Flt1, BCR-ABL, Fyn, Src, and CDK1 (IC50: 18-260 nM). While in normal cells, such as HFL, PrEC, HMEC, and HUVEC, Rigosertib has little or no effect unless its concentration is greater than 5-10 μM. Rigosertib also inhibits several multidrug-resistant tumor cell lines, including MES-SA, MES-SA/DX5a, CEM, and CEM/C2a (IC50: 50-100 nM). Rigosertib (100-250 nM) causes spindle abnormalities and apoptosis in HeLa cells. Rigosertib (0.25-5 μM) blocks cell cycle progression in G2/M phase in DU145 cells, causes an accumulation of cells containing subG1 content of DNA and activates apoptotic pathways. Rigosertib (50 nM-0.5 μM) induces loss of viability and caspase 3/7 activation in A549 cells. Rigosertib sodium (2 μM) induces apoptosis in chronic lymphocytic leukemia (CLL) cells without toxicity against T-cells or normal B-cells. Rigosertib sodium (2 μM) also abrogates the pro-survival effect of follicular dendritic cells on CLL cells and reduces the SDF-1-induced migration of leukemic cells[3][4][5].
In vivo Rigosertib (200 mg/kg, i.p.) displays inhibition on tumor growth in a mouse xenograft model of BT20 cells. Rigosertib (250 mg/kg, i.p.) markedly suppresses tumor growth in mouse xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells [3][4].
Synonyms PI3K, Polo-like Kinase (PLK), Rigosertib, Phosphoinositide 3-kinase, Apoptosis, ON 01910, Inhibitor, ON-01910, inhibit, ON01910
Molecular Weight 451.49
Formula C21H25NO8S
CAS No. 592542-59-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 75 mg/mL (166.12 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Preclinical Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Cell Cycle Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Apoptosis Compound Library

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