Rigosertib (Synonyms: ON-01910)

Name: Rigosertib
Brand: MedChemExpress
SKU: HY-12037A
Rating: 5.0 (5 reviews)

Cat. No.: HY-12037A Purity: 98.52%: FAQs
Data Sheet SDS COA Handling Instructions

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Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM.

For research use only. We do not sell to patients.

Rigosertib Chemical Structure

CAS No. : 592542-59-1

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Rigosertib:

Rigosertib sodium In-stock
(E/Z)-Rigosertib sodium Get quote

5 Publications Citing Use of MCE Rigosertib

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View All Polo-like Kinase (PLK) Isoform Specific Products:

View All Isoforms

PLK1 PLK2 PLK3 PLK4

View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle^[1]^[2]. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM^[3].

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)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	0.062 μM Compound: ON01910	Antiproliferative activity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]
DU-145	GI₅₀	0.075 μM Compound: ON01910	Antiproliferative activity against AR negative human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against AR negative human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]
DU-145	IC₅₀	0.075 μM Compound: 27a	Cytotoxicity against human DU145 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human DU145 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HCT-116	GI₅₀	0.05 μM Compound: 3j	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 21463944]
HCT-116	GI₅₀	0.07 μM Compound: ON01910	Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]
HeLa	GI₅₀	0.012 μM Compound: ON01910	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]
K562	IC₅₀	0.0075 μM Compound: 27a	Cytotoxicity against human K562 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human K562 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
LNCaP	GI₅₀	0.025 μM Compound: ON01910	Antiproliferative activity against AR positive human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against AR positive human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]
MCF7	GI₅₀	0.05 μM Compound: 3j	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 21463944]
MCF7	GI₅₀	0.05 μM Compound: ON01910	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]
MCF7	GI₅₀	0.05 μM Compound: ON01910	Antiproliferative activity against ER positive human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against ER positive human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]
MDA-MB-231	GI₅₀	0.057 μM Compound: ON01910	Antiproliferative activity against ER negative human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against ER negative human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]
MDA-MB-468	GI₅₀	0.02 μM Compound: 3j	Cytotoxicity against human MDA468 cells after 72 hrs by MTT assay Cytotoxicity against human MDA468 cells after 72 hrs by MTT assay	[PMID: 21463944]
MDA-MB-468	GI₅₀	0.302 μM Compound: 3j	Cytotoxicity against human MDA468 cells after 48 hrs by MTT assay Cytotoxicity against human MDA468 cells after 48 hrs by MTT assay	[PMID: 21463944]
MDA-MB-468	GI₅₀	0.601 μM Compound: 3j	Cytotoxicity against human MDA468 cells after 24 hrs by MTT assay Cytotoxicity against human MDA468 cells after 24 hrs by MTT assay	[PMID: 21463944]
MRC5	GI₅₀	0.71 μM Compound: 3j	Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay	[PMID: 21463944]
PANC-1	GI₅₀	0.039 μM Compound: ON01910	Antiproliferative activity against human PANC1 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human PANC1 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]
T47D	GI₅₀	< 0.01 μM Compound: 3j	Cytotoxicity against human T47D cells after 72 hrs by MTT assay Cytotoxicity against human T47D cells after 72 hrs by MTT assay	[PMID: 21463944]
WI-38	GI₅₀	> 10 μM Compound: ON01910	Antiproliferative activity against human WI38 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human WI38 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 24471873]

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^[3]. 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^[4]. 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^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[3]. Rigosertib (200 mg/kg, i.p.) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

451.49

Formula

C₂₁H₂₅NO₈S

CAS No.

592542-59-1

Appearance

Solid

Color

White to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

DMSO : 75 mg/mL (166.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2149 mL	11.0744 mL	22.1489 mL
5 mM	0.4430 mL	2.2149 mL	4.4298 mL
10 mM	0.2215 mL	1.1074 mL	2.2149 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.54 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.52%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (247 KB) HNMR (277 KB) CNMR (277 KB) RP-HPLC (259 KB) LCMS (105 KB)

Handling Instructions (2659 KB)

References

[1]. Xu F, et al. Rigosertib as a selective anti-tumor agent can ameliorate multiple dysregulated signalingtransduction pathways in high-grade myelodysplastic syndrome. Sci Rep. 2014 Dec 4;4:7310. [Content Brief]

[2]. Hyoda T, et al. Rigosertib induces cell death of a myelodysplastic syndrome-derived cell line by DNA damage-induced G2/M arrest. Cancer Sci. 2015 Mar;106(3):287-93. [Content Brief]

[3]. Gumireddy K, et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell. 2005 Mar;7(3):275-86. [Content Brief]

[4]. Reddy MV, et al. Discovery of a clinical stage multi-kinase inhibitor sodium (E)-2-{2-methoxy-5-[(2',4',6'-trimethoxystyrylsulfonyl)methyl]phenylamino}acetate (ON 01910.Na): synthesis, structure-activity relationship, and biological activity. J Med Chem. [Content Brief]

[5]. Chapman CM, et al. ON 01910.Na is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Clin Cancer Res. 2012 Apr 1;18(7):1979-91 [Content Brief]

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]	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]	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 NSC 266046 (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	[1]. Xu F, et al. Rigosertib as a selective anti-tumor agent can ameliorate multiple dysregulated signalingtransduction pathways in high-grade myelodysplastic syndrome. Sci Rep. 2014 Dec 4;4:7310. [Content Brief] [2]. Hyoda T, et al. Rigosertib induces cell death of a myelodysplastic syndrome-derived cell line by DNA damage-induced G2/M arrest. Cancer Sci. 2015 Mar;106(3):287-93. [Content Brief] [3]. Gumireddy K, et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell. 2005 Mar;7(3):275-86. [Content Brief] [4]. Reddy MV, et al. Discovery of a clinical stage multi-kinase inhibitor sodium (E)-2-{2-methoxy-5-[(2',4',6'-trimethoxystyrylsulfonyl)methyl]phenylamino}acetate (ON 01910.Na): synthesis, structure-activity relationship, and biological activity. J Med Chem. [Content Brief] [5]. Chapman CM, et al. ON 01910.Na is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Clin Cancer Res. 2012 Apr 1;18(7):1979-91 [Content Brief]

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2149 mL	11.0744 mL	22.1489 mL	55.3722 mL
	5 mM	0.4430 mL	2.2149 mL	4.4298 mL	11.0744 mL
	10 mM	0.2215 mL	1.1074 mL	2.2149 mL	5.5372 mL
	15 mM	0.1477 mL	0.7383 mL	1.4766 mL	3.6915 mL
	20 mM	0.1107 mL	0.5537 mL	1.1074 mL	2.7686 mL
	25 mM	0.0886 mL	0.4430 mL	0.8860 mL	2.2149 mL
	30 mM	0.0738 mL	0.3691 mL	0.7383 mL	1.8457 mL
	40 mM	0.0554 mL	0.2769 mL	0.5537 mL	1.3843 mL
	50 mM	0.0443 mL	0.2215 mL	0.4430 mL	1.1074 mL
	60 mM	0.0369 mL	0.1846 mL	0.3691 mL	0.9229 mL
	80 mM	0.0277 mL	0.1384 mL	0.2769 mL	0.6922 mL
	100 mM	0.0221 mL	0.1107 mL	0.2215 mL	0.5537 mL

Rigosertib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rigosertib592542-59-1ON-01910ON01910ON 01910Polo-like Kinase (PLK)PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Rigosertib (Synonyms: ON-01910)

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5 Publications Citing Use of MCE Rigosertib

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View All PI3K Isoform Specific Products:

Biological Activity

Protocol

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References

Customer Review

Rigosertib Related Antibodies

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Complete Stock Solution Preparation Table

Rigosertib Related Classifications

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