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Cell Cycle/Checkpoint PLK Rigosertib

Rigosertib

Catalog No. T16750   CAS 592542-59-1
Synonyms: ON-01910

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.

Rigosertib, CAS 592542-59-1
Pack Size Availability Price/USD Quantity
2 mg In stock 53.00
5 mg In stock 76.00
10 mg In stock 130.00
25 mg In stock 298.00
50 mg In stock 486.00
100 mg In stock 803.00
1 mL * 10 mM (in DMSO) In stock 87.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
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 PLK1 : ic50 9 nM,   PLK2 : ic50 260 nM,   PDGFR : ic50 18 nM,   Src : ic50 155 nM,   BCR-ABL : ic50 32 nM,   Cdk1 : ic50 260 nM,   Flt1 : ic50 42 nM,   Fyn : ic50 182 nM,  
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 ON-01910
Purity 98.00%
Molecular Weight 451.49
Formula C21H25NO8S
CAS No. 592542-59-1

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

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

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