Rigosertib (ON-01910)

Catalog No.S1362

Rigosertib (ON-01910) Chemical Structure

Molecular Weight(MW): 473.47

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. Phase 3.

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In DMSO USD 320 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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4 Customer Reviews

  • (A) Rigosertib induced increased apoptosis in CD34+ cells from MDS patients. Especially those from high-grade MDS (Left), in a dose-dependent manner (Right); (B) rigosertib also induced increased apoptosis in MDS and leukemia cell lines, including MDS-L, SKM1, U937, K562, Kasumi-1 and KG1a (Left), in a dose-dependent manner (Right); (C) rigosertib could not induce apoptosis in CD34+ cells from normal controls; (D) the LD50 values were lower in patients with high-grade MDS than in those with low-grade MDS (left). Patients with a normal and abnormal karyotype did not differ;

    Sci Rep, 2014, 4:7310. Rigosertib (ON-01910) purchased from Selleck.

    Along with cell death, immunoblotting shows ON 01910.Na induces hyperphosphorylation of RanGAP1, increased expression of RanGAP1.SUMO1 but decreased expression of free unmodified RanGAP1. No viable SU-DHL-5 cells were available for immunoblotting at 0.5 uM of ON 01910.Na.

    PLoS One 2013 8(11), e79863. Rigosertib (ON-01910) purchased from Selleck.

  • Rigosertib (ON-01910) purchased from Selleck.

    Dr. Antonino Maria Sparta, PhD University of Bologna. Rigosertib (ON-01910) purchased from Selleck.

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Biological Activity

Description 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. Phase 3.
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)
9 nM 18 nM 32 nM 42 nM 155 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human K562 cells MULDfZRwfG:6aXRCpIF{e2G7 NX7DUHR2QTZiaB?= NVvOSGJ2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA6PiCqcoOgZpkhfHK7cHHuJIJtfWViZYjjcJV{cW:wIHHzd4F6NCCLQ{WwQVcvPSCwTR?= MlvYNlE5OTJ2MkG=
human T47D cells NWnLdY1rS3m2b4TvfIlkyqCjc4PhfS=> MX63NkBp NHOzc5dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVPDeGIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9NVAhdk1? MU[yNVQ3Ozl2NB?=
human HeLa cells M4PYVHBzd2yrZnXyZZRqd25iYYPzZZk> NXHGTFRTPzJiaB?= MkXDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0yOiCwTR?= Mk\6NlQ1PzF6N{O=
human MDA468 cells M4nVU2N6fG:2b4jpZ:Kh[XO|YYm= MnfMO|IhcA>? M2jxNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTR4ODDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVIxKG6P NX7IfndPOjF2NkO5OFQ>
human LNCAP cells NIW1Zo9Rem:uaX\ldoF1cW:wIHHzd4F6 NHTZV5g4OiCq M3;KfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRXIheG:|aYTpeoUhcHWvYX6gUG5ESVBiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUK1JI5O MWGyOFQ4OTh5Mx?=
human PANC1 cells MWXQdo9tcW[ncnH0bY9vKGG|c3H5 M3\Re|czKGh? MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCDTlOxJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0{QSCwTR?= MVOyOFQ4OTh5Mx?=
human MCF7 cells MnPYVJJwdGmoZYLheIlwdiCjc4PhfS=> NIrnboQ4OiCq M4\5b2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSXIheG:|aYTpeoUhcHWvYX6gUWNHPyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NUCgcm0> NW\vWFdUOjR2N{G4O|M>
human HCT116 cells MnrNR5l1d3SxeHnjxsBie3OjeR?= NXXncpNiPzJiaB?= NGHjZZBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF02OCCwTR?= MVKyNVQ3Ozl2NB?=
human MCF7 cells Mn[1R5l1d3SxeHnjxsBie3OjeR?= M17zdVczKGh? M4qxcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME21NEBvVQ>? MljLNlE1PjN7NES=
human MDA-MB-231 cells MU\Qdo9tcW[ncnH0bY9vKGG|c3H5 MXe3NkBp M3Xi[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSXIhdmWpYYTpeoUhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[Xl? MYeyOFQ4OTh5Mx?=
human A2780 cells M1TrcHBzd2yrZnXyZZRqd25iYYPzZZk> MoLzO|IhcA>? M{jZV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTZ{IH7N NHHrS5gzPDR5MUi3Ny=>
human HCT116 cells Mn3QVJJwdGmoZYLheIlwdiCjc4PhfS=> M4fPT|czKGh? Ml;YRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTdyIH7N Mo\3NlQ1PzF6N{O=
human DU145 cells MoH2VJJwdGmoZYLheIlwdiCjc4PhfS=> MnmxO|IhcA>? M2TFOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRXIhdmWpYYTpeoUhcHWvYX6gSHUyPDViY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUe1JI5O NH3ZPXgzPDR5MUi3Ny=>
human DU145 cells NH3BW4ZEgXSxdH;4bYPDqGG|c3H5 NVnQWXhEQTZiaB?= NWDXOo5JS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KHS{eYDhckBjdHWnIHX4Z4x2e2mxbjDhd5NigSxiSVO1NF04PSCwTR?= MXiyNVgyOjR{MR?=
human MDA468 cells NVjKWlFRS3m2b4TvfIlkyqCjc4PhfS=> NF\keo41QCCq M4f5RmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTR4ODDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVAvOzB{IN88US=> MkC2NlE1PjN7NES=
human MRC5 cells MYrDfZRwfG:6aXRCpIF{e2G7 MlXpO|IhcA>? Mn7NR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUCuO|Eh|ryP MnnVNlE1PjN7NES=
human A2780 cells MUPGeY5kfGmxbjDhd5NigQ>? NETjS3AxNjJ3IN88US=> NE\wc3kzPCCq MVvS[YR2[3Srb36gbY4hVWOuMTDs[ZZmdCCrbjDoeY1idiCDMke4NEBk\WyuczDheEAxNjJ3IIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NXvOVlhtOjR2N{G4O|M>

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[1]
+ Expand

In vitro enzyme assays for PLK1:

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:[2]
+ Expand
  • 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
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Mouse (female athymic, NCR-nu/nu) xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells
  • Formulation: Dissolved in PBS
  • Dosages: 250 mg/kg
  • Administration: Intraperitonially
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 95 mg/mL (200.64 mM)
Water 95 mg/mL (200.64 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
water
For best results, use promptly after mixing.
95mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 473.47
Formula

C21H24NNaO8S

CAS No. 1225497-78-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00861510 Completed Lymphoma, Mantle-cell|Leukemia, Lymphocytic, Chronic, B-Cell|Leukemia, Hairy Cell|Waldenstrom Macroglobulinemia|Multiple Myeloma National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) March 5, 2009 Phase 1
NCT02730884 Not yet recruiting Leukemia|Myelofibrosis|Anemia|Splenomegaly M.D. Anderson Cancer Center|Onconova Therapeutics, Inc. December 2016 Phase 2
NCT02562443 Recruiting Myelodysplastic Syndrome|MDS|Refractory Anemia With Excess Blasts|RAEB Onconova Therapeutics, Inc. October 2015 Phase 3
NCT02075034 Suspended Myelodysplastic Syndrome Onconova Therapeutics, Inc. May 2014 Phase 1
NCT02030639 Completed Healthy Onconova Therapeutics, Inc. January 2014 Phase 1
NCT02107235 Completed Head and Neck Neoplasms|Carcinoma, Squamous Cell Onconova Therapeutics, Inc. January 2014 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID