Cat. No.: HY-12037A

Rigosertib

Name: Rigosertib
Brand: MedChemExpress
SKU: HY-12037A
Price: 70.00 USD
Availability: InStock
Rating: 5 (6 reviews)

(Synonyms: ON-01910)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

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.

Purity : 97.14%
CAS No.: 592542-59-1
Formula: C₂₁H₂₅NO₈S
Molecular Weight:451.49

Storage:

-20°C, protect from light, stored under nitrogen

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

Rigosertib Chemical Structure

CAS No.: 592542-59-1

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
- In Vivo
Protocols (12)
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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)

All Polo-like Kinase (PLK) Isoforms :

All PI3K Isoforms :

All Raf Isoforms :

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]
A-431	IC₅₀	0.36 μM Compound: Rigosertib	Cytotoxicity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
A549	IC₅₀	0.37 μM Compound: Rigosertib	Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
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]
HeLa S3	EC₅₀	45 nM Compound: Chemical probe : ON01910	Antiproliferative activity against human HeLa S3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human HeLa S3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
HepG2	IC₅₀	1.34 μM Compound: Rigosertib	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
HT-29	IC₅₀	0.16 μM Compound: Rigosertib	Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
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]
K562	IC₅₀	0.15 μM Compound: Rigosertib	Cytotoxicity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
L02	IC₅₀	>40 μM Compound: Rigosertib	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
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 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]
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	IC₅₀	0.26 μM Compound: Rigosertib	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
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]
MV4-11	IC₅₀	1.15 μM Compound: Rigosertib	Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
NCI-H1975	IC₅₀	0.23 μM Compound: Rigosertib	Cytotoxicity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
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]
PANC-1	IC₅₀	0.26 μM Compound: Rigosertib	Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
SGC-7901	IC₅₀	0.25 μM Compound: Rigosertib	Cytotoxicity against human SGC-7901 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human SGC-7901 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38261411]
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. Further protocols information, click here.

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.

Chemical Information

CAS No. 592542-59-1
Appearance Solid
Molecular Weight 451.49
Formula C₂₁H₂₅NO₈S
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
Synonyms

ON-01910
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

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

Publications (6)

All

Sort by:

Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cancer Lett

GPI inactivation mediates pentose phosphate pathway flux switch-on inducing temozolomide resistance in glioma stem cell. [Abstract]

2026 May 1:645:218384. PMID: 41763452
Int J Biol Sci

Glucocorticoids improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels. [Abstract]

2020 Jun 27;16(13):2382-2391. PMID: 32760206
Oncogenesis

STAG2 expression imparts distinct therapeutic vulnerabilities in muscle-invasive bladder cancer cells. [Abstract]

2025 Mar 1;14(1):4. PMID: 40025053
Sci Rep

Identification of Polo-like kinases as potential novel drug targets for influenza A virus. [Abstract]

2017 Aug 17;7(1):8629. PMID: 28819179
Oncol Res

Therapeutic Targeting PLK1 by ON-01910.Na Is Effective in Local Treatment of Retinoblastoma. [Abstract]

2021 Sep 7;28(7):745-761. PMID: 33573708

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocols

All Signal Pathway Related Molecular Biology Cell Biology

Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of ³²P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
Directly Induced Neuron Culture
Directly induced neuron culture converts somatic cells, most commonly fibroblasts, into induced neurons without passing through a pluripotent or neural progenitor stage; classic evidence shows that mouse fibroblasts can be converted by Ascl1, Brn2/Pou3f2, and Myt1l, human fibroblasts can be converted by defined neuronal transcription factors, and human fibroblasts can also be converted by miR-9/9-124 with neurogenic or subtype-specifying transcription factors. The readout is acquisition of neuronal identity and function, assessed by neuronal morphology, neuronal markers such as Tuj1/βIII-tubulin, MAP2, synapsin, and subtype markers when relevant, together with functional assays such as action-potential firing, synaptic activity, and electrophysiology.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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. 2011 Sep 22;54(18):6254-76. [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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Rigosertib

Publications Citing Use of MedChemExpress (MCE) Rigosertib

All Polo-like Kinase (PLK) Isoforms

All PI3K Isoforms

All Raf Isoforms