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

Rigosertib sodium (Synonyms: ON-01910 sodium; ON01910 sodium; ON01910 sodium)

Cat. No.: HY-12037 Purity: 99.09%
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.

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Rigosertib sodium Chemical Structure

Rigosertib sodium Chemical Structure

CAS No. : 592542-60-4

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Other Forms of Rigosertib sodium:

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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
Sponsor Condition Start Date Phase
Onconova Therapeutics Inc Myelodysplastic syndrome 2013-08-31 Safety; Efficacy; Pharmacokinetics
Onconova Therapeutics Inc Metastatic pancreas cancer 2011-05-31 Safety; Efficacy; Pharmacokinetics; Pharmacodynamics
Onconova Therapeutics Inc Myelodysplastic syndrome 2010-11-30 Safety; Efficacy
Onconova Therapeutics Inc Myelodysplastic syndrome 2013-07-31 Safety; Efficacy
Stanford University Myelodysplastic syndrome 2009-05-31 Safety; Efficacy
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.

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.

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

Purity: 99.09%

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Rigosertib sodium
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HY-12037
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