1. Cell Cycle/DNA Damage
  2. Polo-like Kinase (PLK)

Rigosertib sodium (Synonyms: ON-01910 sodium)

Cat. No.: HY-12037 Purity: 99.09%
Data Sheet SDS Handling Instructions

Rigosertib (sodium) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM, and shows 30-fold greater selectivity against PLK2.

For research use only. We do not sell to patients.
Rigosertib sodium Chemical Structure

Rigosertib sodium Chemical Structure

CAS No. : 592542-60-4

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Description

Rigosertib (sodium) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM, and shows 30-fold greater selectivity against PLK2.

IC50 & Target

IC50: 9 nM (PLK1)

In Vitro

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[1]. 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[2]. 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[3].

In Vivo

Rigosertib (250 mg/kg) markedly inhibits tumor growth in mouse xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells[1]. Rigosertib (200 mg/kg) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01048619 Onconova Therapeutics, Inc. Myelodysplastic Syndrome December 2009 Phase 1
NCT00854646 Onconova Therapeutics, Inc. Acute Myelocytic Leukemia|Acute Lymphocytic Leukemia|Chronic Myelocytic Leukemia|Chronic Lymphocytic Leukemia|Myelodysplastic Syndromes October 2008 Phase 1
NCT00854945 Onconova Therapeutics, Inc. Myelodysplastic Syndrome|Acute Myeloid Leukemia January 2009 Phase 1|Phase 2
NCT01125891 Onconova Therapeutics, Inc. Malignant Neoplasmas|Solid Tumors January 2009 Phase 1
NCT00856791 Onconova Therapeutics, Inc. Ovarian Cancer March 2009 Phase 2
NCT01241500 Onconova Therapeutics, Inc.|The Leukemia and Lymphoma Society Myelodysplastic Syndromes|MDS|RAEB|Chronic Myelomonocytic Leukemia November 2010 Phase 3
NCT00906334 Onconova Therapeutics, Inc. Myelodysplastic Syndrome May 2009 Phase 2
NCT00861328 Onconova Therapeutics, Inc. Advanced Solid Tumors February 2008 Phase 1
NCT00861783 Onconova Therapeutics, Inc. Hepatoma|Advanced Solid Tumor June 2008 Phase 1
NCT01360853 Onconova Therapeutics, Inc.|Academic Oncology Gastrointestinal Cancer Consortium (AGICC) Metastatic Pancreatic Adenocarcinoma May 2011 Phase 3
NCT01165905 Onconova Therapeutics, Inc. Solid Tumor January 2010 Phase 1
NCT00867061 Onconova Therapeutics, Inc. Myelodysplastic Syndrome March 2009 Phase 1|Phase 2
NCT00533416 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Myelodysplastic Syndrome (MDS) September 14, 2007 Phase 1
NCT00861510 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Lymphoma, Mantle-cell|Leukemia, Lymphocytic, Chronic, B-Cell|Leukemia, Hairy Cell|Waldenstrom Macroglobulinemia|Multiple Myeloma March 5, 2009 Phase 1
NCT01168011 Onconova Therapeutics, Inc. Solid Tumor July 2010 Phase 1
NCT01167166 Onconova Therapeutics, Inc. Acute Myelocytic Leukemia|Acute Lymphocytic Leukemia|Myeloproliferative Disease|Chronic Myeloid Leukemia July 2010 Phase 1|Phase 2
NCT01807546 Onconova Therapeutics, Inc. Head and Neck Squamous Cell Carcinoma|Anal Squamous Cell Carcinoma|Lung Squamous Cell Carcinoma|Cervical Squamous Cell Carcinoma|Esophageal Squamous Cell Carcinoma|Skin Squamous Cell Carcinoma|Penile Squamous Cell Carcinoma March 2013 Phase 2
NCT02030639 Onconova Therapeutics, Inc. Healthy January 2014 Phase 1
NCT01904682 Onconova Therapeutics, Inc. Myelodysplastic Syndromes July 2013 Phase 2
NCT01584531 Onconova Therapeutics, Inc. Myelodysplastic Syndrome|MDS|Trisomy 8 May 2012 Phase 2
NCT02075034 Onconova Therapeutics, Inc. Myelodysplastic Syndrome May 2014 Phase 1
NCT01926587 Onconova Therapeutics, Inc. Myelodysplastic Syndrome|Acute Myeloid Leukemia|Chronic Myelomonocytic Leukemia August 2013 Phase 2
NCT02730884 M.D. Anderson Cancer Center|Onconova Therapeutics, Inc. Leukemia|Myelofibrosis|Anemia|Splenomegaly September 2017 Phase 2
NCT01928537 Onconova Therapeutics, Inc. Myelodysplastic Syndromes|Refractory Anemia With Excess Blasts|Chronic Myelomonocytic Leukemia|Cytopenia August 2013 Phase 3
NCT02107235 Onconova Therapeutics, Inc. Head and Neck Neoplasms|Carcinoma, Squamous Cell January 2014 Phase 1
NCT01538537 Onconova Therapeutics, Inc. Advanced Cancer|Solid Tumors|Cancer|Neoplasms August 2006 Phase 1
NCT01538563 Onconova Therapeutics, Inc. Solid Tumors|Advanced Cancer|Cancer|Neoplasms June 2006 Phase 1
NCT02562443 Onconova Therapeutics, Inc. Myelodysplastic Syndrome|MDS|Refractory Anemia With Excess Blasts|RAEB October 2015 Phase 3
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References
Kinase Assay
[1]

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

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 1×105 cells/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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
M.Wt

473.47

Formula

C₂₁H₂₄NNaO₈S

CAS No.

592542-60-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

H2O: ≥ 52 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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