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Rigosertib (ON-01910)
Catalog No.S1362
For research use only.
Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.
CAS No. 1225497-78-8
Selleck's Rigosertib (ON-01910) has been cited by 29 publications
Purity & Quality Control
Choose Selective PLK Inhibitors
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Biological Activity
| Description | Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| In vivo | In mouse xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells, Rigosertib (250 mg/kg) markedly inhibits tumor growth. [1] Rigosertib (200 mg/kg) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells. [2] |
Protocol (from reference)
| Kinase Assay:[1] |
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| Cell Research:[2] |
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| Animal Research:[1] |
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| References |
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Solubility (25°C)
|
In vitro |
DMSO |
95 mg/mL
(200.64 mM) |
| Water |
95 mg/mL
(200.64 mM) |
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| Ethanol |
Insoluble
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In vivo |
Add solvents to the product individually and in order |
95mg/mL |
Chemical Information
| Molecular Weight | 473.47 | ||
|---|---|---|---|
| Formula | C21H24NNaO8S |
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| CAS No. | 1225497-78-8 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | COC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)[O-].[Na+] | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04177498 | Recruiting | Drug: Rigosertib Sodium|Other: Quality-of-Life Assessment | Recessive Dystrophic Epidermolysis Bullosa | Thomas Jefferson University|Onconova Therapeutics Inc. | August 24 2021 | Early Phase 1 |
| NCT02075034 | Withdrawn | Drug: rigosertib | Myelodysplastic Syndrome | Onconova Therapeutics Inc. | May 2014 | Phase 1 |
| NCT02030639 | Completed | Drug: rigosertib | Healthy | Onconova Therapeutics Inc. | January 2014 | Phase 1 |
| NCT01928537 | Completed | Drug: rigosertib sodium | Myelodysplastic Syndromes|Refractory Anemia With Excess Blasts|Chronic Myelomonocytic Leukemia|Cytopenia | Onconova Therapeutics Inc. | August 2013 | Phase 3 |
| NCT01807546 | Completed | Drug: rigosertib | 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 | Onconova Therapeutics Inc. | March 2013 | Phase 2 |
| NCT01168011 | Completed | Drug: rigosertib | Solid Tumor | Onconova Therapeutics Inc. | July 2010 | Phase 1 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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