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    Rigosertib sodium (ON-01910)
    Rigosertib sodium (ON-01910)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1575
    CAS #: 1225497-78-8 Purity ≥98%

    Description: Rigosertib sodium (formerly known as ON-01910; ON01910; Estybon), the sodium salt of Rigosertib, is a novel, potent and non-ATP-competitive inhibitor of PLK1 with potential anticancer activity. It inhibits PLK1 with an IC50 of 9 nM in a cell-free assay. Rigosertib shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib can be potentially used for the treatment of cancer. Rigosertib inhibits polo-like kinase1 (Plk1), inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. This agent may exhibit synergistic antitumor activity in combination with other chemotherapeutic agents. 

    References: Cancer Cell. 2005 Mar;7(3):275-86; J Med Chem. 2011 Sep 22;54(18):6254-76.

    Related CAS#: 592542-59-1 (free acid); 1225497-78-8 or 592542-60-4 (sodium)

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    Molecular Weight (MW)473.47
    FormulaC21H24NNaO8S
    CAS No.1225497-78-8 (sodium); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 95 mg/mL (200.6 mM)
    Water: 95 mg/mL (200.6 mM)
    Ethanol: <1 mg/mL
    Solubility (In vivo)Saline: 30 mg/mL
    SynonymsON-01910; Rigosertib sodium; ON01910; ON 01910; brand name: Estybon


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    In Vitro

    In vitro activity: Rigosertib is non-ATP-competitive inhibitor to PLK1 with IC50 of 9 nM. Rigosertib also exhibits inhibition against PLK2, PDGFR, Flt1, BCR-ABL, Fyn, Src, and CDK1, with IC50 of 18-260 nM. Rigosertib shows cell killing activity against 94 different tumor cell lines with IC50 of 50-250 nM, including BT27, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, SW480, and KB cells. 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. In HeLa cells, Rigosertib (100-250 nM) induces spindle abnormalities and apoptosis. Rigosertib also inhibits several multidrug resistant tumor cell lines, including MES-SA, MES-SA/DX5a, CEM, and CEM/C2a, with IC50 of 50-100 nM. In DU145 cells, Rigosertib (0.25-5 μM) blocks cell cycle progression in G2/M phase, results in an accumulation of cells containing subG1 content of DNA, and activates apoptotic pathways. In A549 cells, Rigosertib (50 nM-0.5 μM) induces loss of viability and caspase 3/7 activation. In a recent study, Rigosertib induces apoptosis in chronic lymphocytic leukemia (CLL) cells without toxicity against T-cells or normal B-cells. Rigosertib also abrogates the pro-survival effect of follicular dendritic cells on CLL cells and reduces SDF-1-induced migration of leukemic cells.


    Kinase Assay: Recombinant PLK1 (10 ng) is incubated with different concentrations of Rigosertib in a 15 µL reaction mixture (50 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 2 mM Dithiothreitol, 0.01% NP-40 [pH 7.5]) for 30 min at room temperature. Kinase reactions are performed for 20 min at 30 °C in a volume of 20 µL (15 µL enzyme + inhibitor, 2 µL 1 mM ATP), 2 µL of γ32P-ATP (40 μCi), and 1 µL of recombinant Cdc25C (100 ng) or casein (1 μg) substrates. Reactions are terminated by boiling for 2 min in 20 µL of 2× Laemmli buffer. Phosphorylated substrates are separated by 18% SDS-PAGE. The gels are dried and exposed to X-ray film for 3-10 min.


    Cell Assay: Cells (A number of tumor cell lines, including BT20, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, HeLa, and Raji cells) are grown in either DMEM or RPMI supplemented with 10% fetal bovine serum and 1 unit/mL penicillin-streptomycin solution. Tumor cells are plated into six-well dishes at a density of 1 × 105cells/mL/well, and Rigosertib is added 24 hours later at various concentrations. Cell counts are determined from duplicate wells after 96-hour of treatment. The total number of viable cells is determined by trypan blue exclusion.

    In VivoIn mouse xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells, Rigosertib (250 mg/kg) markedly inhibits tumor growth. Rigosertib (200 mg/kg) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells.
    Animal modelMouse (female athymic, NCR-nu/nu) xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells
    Formulation & DosageDissolved in PBS; 250 mg/kg; i.p. injection
    References

    Cancer Cell. 2005 Mar;7(3):275-86; J Med Chem. 2011 Sep 22;54(18):6254-76.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Rigosertib (ON-01910)

    28 (ON 01910.Na) selectively induces mitotic G2/M arrest and apoptosis in cancer cells.  2011 Sep 22;54(18):6254-76.

     

    Rigosertib (ON-01910)

    DU145 and HFL-1 (normal human fibroblasts) cells were treated with increasing concentrations of 28 or DMSO (Vehicle) for 48 h.  2011 Sep 22;54(18):6254-76.

     

    Rigosertib (ON-01910)

    Cellular viability together with the activity of caspases 3/7 were assayed concomitantly in A549 cells treated with 28 for 24 h (n=3).  2011 Sep 22;54(18):6254-76.


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