2. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
    Apoptosis
  3. Polo-like Kinase (PLK)
    PI3K
    Apoptosis
  4. Rigosertib

Rigosertib  (Synonyms: ON-01910)

Cat. No.: HY-12037A Purity: 98.09%
COA Handling Instructions

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

Rigosertib Chemical Structure

CAS No. : 592542-59-1

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5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
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100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Rigosertib:

Top Publications Citing Use of Products

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PLK1 PLK2 PLK3 PLK4

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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)

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

451.49

Appearance

Solid

Formula

C21H25NO8S
CAS No.
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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.09%

COA (246 KB) HNMR (210 KB) RP-HPLC (146 KB) LCMS (125 KB)

Handling Instructions (2659 KB)
References
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
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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.

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Keywords:

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

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