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Rigosertib (ON-01910)

Name: Rigosertib (ON-01910)
Brand: Selleck Chemicals
SKU: S1362
Rating: 5 (34 reviews)

Catalog No.S1362 Purity:99.52%

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

CAS No. 1225497-78-8

Purity & Quality Control

Batch: Purity: 99.52%

99.52

Rigosertib (ON-01910) Related Products

Related Targets	PLK1 PLK2 PLK3 PLK4	Click to Expand
Related Products	BI 2536 Volasertib GSK461364 Onvansertib (NMS-P937) SBE 13 HCl Ro3280 CFI-400945 HMN-214 MLN0905 Poloxin	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	Click to Expand

Signaling Pathway

PLK Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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

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	Click to View More Targets

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
Kinase Assay	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Clear solution	saline	94.000mg/ml (198.53mM)	Taking the 1 mL working solution as an example, add 94 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	saline	95.000mg/ml (200.65mM)	Taking the 1 mL working solution as an example, add 95 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	saline	95.000mg/ml (200.65mM)	Taking the 1 mL working solution as an example, add 95 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	water Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	95.000mg/ml (200.65mM)	Taking the 1 mL working solution as an example, add 95 mg of this product to 1 ml of ddH2O, mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	saline	95.000mg/ml (200.65mM)	Taking the 1 mL working solution as an example, add 95 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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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.
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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

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