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

Rigosertib sodium (Synonyms: ON-01910 sodium)

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

Rigosertib (sodium) is a non-ATP-competitive inhibitor of PLK1 with an 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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10 mM * 1 mL in Water USD 92 In-stock
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Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
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10 mg USD 144 In-stock
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Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
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Estimated Time of Arrival: December 31
100 mg USD 900 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Other Forms of Rigosertib sodium:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[1]

PLK1

9 nM (IC50)

PLK2

260 nM (IC50)

PDGFR

18 nM (IC50)

Src

155 nM (IC50)

BCR-ABL

32 nM (IC50)

Cdk1

260 nM (IC50)

Flt1

42 nM (IC50)

Fyn

182 nM (IC50)

In Vitro

Rigosertib is non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM. Rigosertib also exhibits inhibition of 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]. 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 SDF-1-induced migration of leukemic cells[3].

In Vivo

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

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.1121 mL 10.5603 mL 21.1207 mL
5 mM 0.4224 mL 2.1121 mL 4.2241 mL
10 mM 0.2112 mL 1.0560 mL 2.1121 mL
Please refer to the solubility information to select the appropriate solvent.
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.

Animal Administration
[1]

Rigosertib is dissolved in dissolved in PBS.

Bel-7402 tumor models: twenty female athymic (NCR-nu/nu) nude mice are injected with 1 × 107 Bel-7402 tumor cells subcutaneously, and 10-14 days later, when the tumor volumes reach 200-250 mm, the mice are divided into four groups such that each group harbors tumors of the same volume. Rigosertib (ON01910, 250 mg/kg) dissolved in PBS is administered alone or in combination with oxaliplatin (100 mg/kg) intraperitonially on alternate days. Tumor measurements are done two times/week using traceable digital vernier calipers. Body weight is determined during each measurement. The animals are observed for signs of toxicity[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

473.47

Formula

C₂₁H₂₄NNaO₈S

CAS No.

592542-60-4

SMILES

COC1=CC=C(C=C1NCC([O-])=O)CS(/C=C/C2=C(C=C(C=C2OC)OC)OC)(=O)=O.[Na+]

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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Rigosertib sodium
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