Cat. No.: HY-12037

Rigosertib sodium

(Synonyms: ON-01910 sodium)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib sodium 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: 99.57%
CAS No.: 592542-60-4
Formula: C₂₁H₂₄NNaO₈S
Molecular Weight:473.47

Storage:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Rigosertib sodium Chemical Structure

CAS No.: 592542-60-4

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
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Bioz

Biological Activity

Description

Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle^[1]^[2]. Rigosertib sodium 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 :

Cellular Effect

Cell Line	Type	Value	Description	References
2008	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human 2008 cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against human 2008 cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
A2780	GI₅₀	0.04 μM Compound: Rigosertib Sodium	Antiproliferative activity against human A2780 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A2780 cells measured after 72 hrs by MTT assay	[PMID: 27815119]
A549	IC₅₀	0.09 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human A549 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human A549 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
AGS	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human AGS cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human AGS cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
Bel-7402	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human Bel7402 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human Bel7402 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
BT-20	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human BT20 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human BT20 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
BT-474	IC₅₀	0.05 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human BT474 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human BT474 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
BXPC-3	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human BxPC3 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human BxPC3 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
CCRF-CEM	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human CEM cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against human CEM cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
CEM/C2	IC₅₀	0.05 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against multidrug-resistant human CEM/C2 cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against multidrug-resistant human CEM/C2 cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
COLO 205	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human COLO205 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human COLO205 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
COLO 320	IC₅₀	0.06 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human COLO320 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human COLO320 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
Daudi	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human Daudi cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human Daudi cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
DLD-1	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human DLD1 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human DLD1 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
DU-145	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	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]
Granta-519	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human GRANTA-519 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human GRANTA-519 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HCC70	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HCC70 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HCC70 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HCT-116	GI₅₀	0.06 μM Compound: Rigosertib Sodium	Antiproliferative activity against human HCT116 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells measured after 72 hrs by MTT assay	[PMID: 27815119]
HCT-116	IC₅₀	0.01 μM Compound: 1; ON01910	Cytotoxicity against human HCT-116 cells Cytotoxicity against human HCT-116 cells	[PMID: 35305462]
HCT-116	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HCT116 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HCT116 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HCT-15	IC₅₀	0.09 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HCT15 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HCT15 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HEL	IC₅₀	0.05 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HEL cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HEL cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HeLa	IC₅₀	0.01 μM Compound: 1; ON01910	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 35305462]
HeLa	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HeLa cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HeLa cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HepG2	IC₅₀	0.01 μM Compound: 1; ON01910	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 35305462]
HL-60	IC₅₀	0.02 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human HL60 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human HL60 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
HUVEC	IC₅₀	>100 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against HUVEC after 96 hrs by trypan blue exclusion assay Cytotoxicity against HUVEC after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
K562	IC₅₀	0.015 μM Compound: 28, ON 01910.Na, ESTYBON	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]
KB	IC₅₀	0.07 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human KB cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human KB cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
KG-1a	IC₅₀	0.03 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human KG1a cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human KG1a cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
LP-1	IC₅₀	0.03 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human LP-1 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human LP-1 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MCF7	IC₅₀	0.01 μM Compound: 1; ON01910	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 35305462]
MCF7	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MCF7 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MCF7 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MDA-MB-157	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MDA-MB-157 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MDA-MB-157 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MDA-MB-231	IC₅₀	0.025 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MDA-MB-231 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MDA-MB-231 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MES-SA	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MES-SA cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against human MES-SA cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
MES-SA/Dx5	IC₅₀	0.1 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against multidrug-resistant human MES-SA/Dx5 cells assessed as cell viability after 96 hrs by trypan blue exclusion Cytotoxicity against multidrug-resistant human MES-SA/Dx5 cells assessed as cell viability after 96 hrs by trypan blue exclusion	[PMID: 21812421]
MIA PaCa-2	IC₅₀	0.05 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MIAPaCa2 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MIAPaCa2 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
MOLT-4	IC₅₀	0.04 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human MOLT4 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human MOLT4 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NAMALVA	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NAMALWA cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NAMALWA cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NCI-H1299	IC₅₀	0.01 μM Compound: 1; ON01910	Cytotoxicity against human NCI-H1299 cells Cytotoxicity against human NCI-H1299 cells	[PMID: 35305462]
NCI-H157	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NCI-H157 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NCI-H157 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NCI-H187	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NCI-H187 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NCI-H187 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NCI-H1975	IC₅₀	0.09 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NCI-H1975 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NCI-H1975 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
NCI-H417	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human NCI-N417 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human NCI-N417 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
OPM-2	IC₅₀	0.015 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human OPM2 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human OPM2 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
OVCAR-3	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human OVCAR3 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human OVCAR3 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
PANC-1	IC₅₀	0.04 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human PANC1 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human PANC1 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
PC-3	IC₅₀	0.15 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human PC3 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human PC3 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
Raji	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human Raji cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human Raji cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
RPMI-7951	IC₅₀	0.025 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human RPMI7951 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human RPMI7951 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
SK-BR-3	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human SKBR3 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human SKBR3 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
SW480	IC₅₀	0.06 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human SW480 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human SW480 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
T47D	IC₅₀	0.17 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human T47D cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human T47D cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
U-266	IC₅₀	0.025 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human U266 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human U266 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
U-87MG ATCC	IC₅₀	0.08 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human U87 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human U87 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
U-937	IC₅₀	0.01 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human U937 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human U937 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]
WM793	IC₅₀	0.075 μM Compound: 28, ON 01910.Na, ESTYBON	Cytotoxicity against human WM793 cells after 96 hrs by trypan blue exclusion assay Cytotoxicity against human WM793 cells after 96 hrs by trypan blue exclusion assay	[PMID: 21812421]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 592542-60-4
Appearance Solid
Molecular Weight 473.47
Formula C₂₁H₂₄NNaO₈S
Color White to yellow
SMILES

COC1=CC=C(C=C1NCC(O[Na])=O)CS(/C=C/C2=C(C=C(C=C2OC)OC)OC)(=O)=O
Synonyms

ON-01910 sodium
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (6)

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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
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
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

Solvent & Solubility

In Vitro:

DMSO : 150 mg/mL (316.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 52 mg/mL (109.83 mM)

* "≥" means soluble, but saturation unknown.

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

2.1121 mL

10.5603 mL

21.1207 mL

5 mM

0.4224 mL

2.1121 mL

4.2241 mL

10 mM

0.2112 mL

1.0560 mL

2.1121 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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)

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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: ≥ 5.25 mg/mL (11.09 mM); Clear solution

This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 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: ≥ 5.25 mg/mL (11.09 mM); Clear solution

This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 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: ≥ 5.25 mg/mL (11.09 mM); Clear solution

This protocol yields a clear solution of ≥ 5.25 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 (52.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (5.28 mM); Suspended solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: PBS

Solubility: 50 mg/mL (105.60 mM); Clear solution; Need ultrasonic

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.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Protocol

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.

MedChemExpress (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].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
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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. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.1121 mL	10.5603 mL	21.1207 mL	52.8017 mL
	5 mM	0.4224 mL	2.1121 mL	4.2241 mL	10.5603 mL
	10 mM	0.2112 mL	1.0560 mL	2.1121 mL	5.2802 mL
	15 mM	0.1408 mL	0.7040 mL	1.4080 mL	3.5201 mL
	20 mM	0.1056 mL	0.5280 mL	1.0560 mL	2.6401 mL
	25 mM	0.0845 mL	0.4224 mL	0.8448 mL	2.1121 mL
	30 mM	0.0704 mL	0.3520 mL	0.7040 mL	1.7601 mL
	40 mM	0.0528 mL	0.2640 mL	0.5280 mL	1.3200 mL
	50 mM	0.0422 mL	0.2112 mL	0.4224 mL	1.0560 mL
	60 mM	0.0352 mL	0.1760 mL	0.3520 mL	0.8800 mL
	80 mM	0.0264 mL	0.1320 mL	0.2640 mL	0.6600 mL
	100 mM	0.0211 mL	0.1056 mL	0.2112 mL	0.5280 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Rigosertib sodium

6 Cited Publications

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Rigosertib sodium

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

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Glycolysis Compound Library

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Rare Diseases Drug Library

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Publications Citing Use of MedChemExpress (MCE) Rigosertib sodium

All Polo-like Kinase (PLK) Isoforms

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rigosertib sodium Related Classifications

HY-12037 Related Classifications