Home Cell Cycle PLK inhibitor - PI3K inhibitor - Akt inhibitor - Apoptosis related activator Rigosertib (ON-01910) For research use only.

Rigosertib (ON-01910)

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.

Rigosertib (ON-01910) Chemical Structure

Rigosertib (ON-01910) Chemical Structure

CAS No. 1225497-78-8

Purity & Quality Control

Rigosertib (ON-01910) Related Products

Signaling Pathway

PLK Signaling Pathways

PLK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T47D Cytotoxicity assay 72 hrs Cytotoxicity against human T47D cells after 72 hrs by MTT assay, GI50 = 0.01 μM. 21463944
MDA468 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA468 cells after 72 hrs by MTT assay, GI50 = 0.02 μM. 21463944
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, GI50 = 0.05 μM. 21463944
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, GI50 = 0.05 μM. 21463944
MDA468 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA468 cells after 48 hrs by MTT assay, GI50 = 0.302 μM. 21463944
MDA468 Cytotoxicity assay 24 hrs Cytotoxicity against human MDA468 cells after 24 hrs by MTT assay, GI50 = 0.601 μM. 21463944
MRC5 Cytotoxicity assay 72 hrs Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, GI50 = 0.71 μM. 21463944
MCF7 Function assay 1 uM Metabolic stability of the compound in human MCF7 cells at 1 uM 21463944
MRC5 Function assay 1 uM Metabolic stability of the compound in human MRC5 cells at 1 uM 21463944
K562 Cytotoxicity assay 96 hrs Cytotoxicity against human K562 cells after 96 hrs by trypan blue exclusion assay, IC50 = 0.0075 μM. 21812421
DU145 Cytotoxicity assay 96 hrs Cytotoxicity against human DU145 cells after 96 hrs by trypan blue exclusion assay, IC50 = 0.075 μM. 21812421
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.012 μM. 24471873
LNCAP Antiproliferative assay 72 hrs Antiproliferative activity against AR positive human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.025 μM. 24471873
PANC1 Antiproliferative assay 72 hrs Antiproliferative activity against human PANC1 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.039 μM. 24471873
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against ER positive human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.05 μM. 24471873
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.05 μM. 24471873
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against ER negative human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.057 μM. 24471873
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.062 μM. 24471873
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.07 μM. 24471873
DU145 Antiproliferative assay 72 hrs Antiproliferative activity against AR negative human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.075 μM. 24471873
A2780 Function assay 0.25 uM 24 hrs Reduction in CDC25C level in human A2780 cells at 0.25 uM after 24 hrs by Western blot analysis 24471873
A2780 Apoptosis assay 0.25 uM 24 hrs Induction of apoptosis in human A2780 cells assessed as caspase-3/7 activation at 0.25 uM after 24 hrs by using Apo-ONE homogeneous caspase-3/7 kit 24471873
A2780 Function assay 0.25 uM 24 hrs Reduction in Mcl1 level in human A2780 cells at 0.25 uM after 24 hrs by Western blot analysis 24471873
Click to View More Cell Line Experimental Data

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.
Targets
PLK1 [1]
(Cell-free assay)		 PDGFR [1]
(Cell-free assay)		 Bcr-Abl [1]
(Cell-free assay)		 Flt1 [1]
(Cell-free assay)		 Src [1]
(Cell-free assay)		 Click to View More Targets
9 nM 18 nM 32 nM 42 nM 155 nM
In vitro
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]
Kinase Assay In vitro enzyme assays for PLK1
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 Research Cell lines A number of tumor cell lines, including BT20, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, HeLa, and Raji cells
Concentrations 1 nM - 10 μM, dissolved in DMSO as stock solution.
Incubation Time 96 hours
Method 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 exclusio
Experimental Result Images Methods Biomarkers Images PMID
Western blot pAbl / Abl / PCrk-L / Crk-L / Cleaved caspase3 / Cleaved PARP / pHistone H2A.X 26008977
Immunofluorescence p-ATF / COX IV 27764820
Growth inhibition assay GI50 Cell viability 29108241
In Vivo
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]
Animal Research Animal Models Mouse (female athymic, NCR-nu/nu) xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells
Dosages 250 mg/kg
Administration Intraperitonially
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04177498 Recruiting
Recessive Dystrophic Epidermolysis Bullosa
Thomas Jefferson University|Traws Pharma Inc.
 August 24 2021 Early Phase 1
NCT02075034 Withdrawn
Myelodysplastic Syndrome
Traws Pharma Inc.
 May 2014 Phase 1
NCT02030639 Completed
Healthy
Traws Pharma Inc.
 January 2014 Phase 1
NCT01928537 Completed
Myelodysplastic Syndromes|Refractory Anemia With Excess Blasts|Chronic Myelomonocytic Leukemia|Cytopenia
Traws Pharma Inc.
 August 2013 Phase 3
NCT01807546 Completed
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
Traws Pharma Inc.
 March 2013 Phase 2
NCT01168011 Completed
Solid Tumor
Traws Pharma Inc.
 July 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 473.47 Formula

C21H24NNaO8S
CAS No. 1225497-78-8 SDF Download Rigosertib (ON-01910) SDF
Smiles COC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)[O-].[Na+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (198.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 94 mg/mL

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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
%DMSO %

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.

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Rigosertib (ON-01910) | Rigosertib (ON-01910) supplier | purchase Rigosertib (ON-01910) | Rigosertib (ON-01910) cost | Rigosertib (ON-01910) manufacturer | order Rigosertib (ON-01910) | Rigosertib (ON-01910) distributor