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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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)
9 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 NWL4SGt2S3m2b4TvfIlkyqCjc4PhfS=> M2DtWVk3KGh? MkfKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC5OkBpenNiYomgeJJ6eGGwIHLseYUh\XilbIXzbY9vKGG|c3H5MEBKSzVyPUeuOUBvVQ>? MXKyNVgyOjR{MR?=
human T47D cells M4HnVGN6fG:2b4jpZ:Kh[XO|YYm= NVz6[JdCPzJiaB?= M4O1R2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHQ1P0RiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2xNEBvVQ>? MojkNlE1PjN7NES=
human HeLa cells MVrQdo9tcW[ncnH0bY9vKGG|c3H5 NG\0XGo4OiCq NWixTINCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygS2k2OD1zMjDuUS=> NUG4RXR6OjR2N{G4O|M>
human MDA468 cells NXLmS2JCS3m2b4TvfIlkyqCjc4PhfS=> NYDVPGZvPzJiaB?= MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGE1PjhiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2yNEBvVQ>? MlmyNlE1PjN7NES=
human LNCAP cells MmfQVJJwdGmoZYLheIlwdiCjc4PhfS=> NYDxeYFoPzJiaB?= MlHpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDBVkBxd3OrdHn2[UBpfW2jbjDMUmNCWCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;MkWgcm0> MYiyOFQ4OTh5Mx?=
human PANC1 cells NEPsfHFRem:uaX\ldoF1cW:wIHHzd4F6 NHrDXZc4OiCq NWHrdZloSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQRW5EOSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;M{mgcm0> MYiyOFQ4OTh5Mx?=
human MCF7 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 NHn6UVg4OiCq M{\ITmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSXIheG:|aYTpeoUhcHWvYX6gUWNHPyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NUCgcm0> NX\HVZZTOjR2N{G4O|M>
human HCT116 cells NX[0ZpptS3m2b4TvfIlkyqCjc4PhfS=> MnPkO|IhcA>? NYDUXItMS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFfJOVA:PTBibl2= NGqxWWEzOTR4M{m0OC=>
human MCF7 cells MYrDfZRwfG:6aXRCpIF{e2G7 M2jVOlczKGh? NIjOfYhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9OVAhdk1? NH7ZbpYzOTR4M{m0OC=>
human MDA-MB-231 cells M2LBV3Bzd2yrZnXyZZRqd25iYYPzZZk> NHPU[4U4OiCq NV3BTGh{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBGWiCwZXfheIl3\SCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeR?= Ml\JNlQ1PzF6N{O=
human A2780 cells M{fGdnBzd2yrZnXyZZRqd25iYYPzZZk> M{DiT|czKGh? NIDMfoxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygS2k2OD14MjDuUS=> NVPYPFB2OjR2N{G4O|M>
human HCT116 cells M4q5SHBzd2yrZnXyZZRqd25iYYPzZZk> M1rZb|czKGh? M1r5[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygS2k2OD15MDDuUS=> MlPMNlQ1PzF6N{O=
human DU145 cells NH[yUXJRem:uaX\ldoF1cW:wIHHzd4F6 MYO3NkBp M17HT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRXIhdmWpYYTpeoUhcHWvYX6gSHUyPDViY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUe1JI5O MV2yOFQ4OTh5Mx?=
human DU145 cells NYDIPG9MS3m2b4TvfIlkyqCjc4PhfS=> NWHIWFYzQTZiaB?= Mk[5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgPVYhcHK|IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCjc4PhfUwhUUN3ME23OUBvVQ>? NG\leJgzOThzMkSyNS=>
human MDA468 cells MXvDfZRwfG:6aXRCpIF{e2G7 NUnv[YdyPDhiaB?= NF;LcpJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEF2NkigZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0xNjNyMjFOwG0> NFTMSWUzOTR4M{m0OC=>
human MRC5 cells NWHWd4d7S3m2b4TvfIlkyqCjc4PhfS=> M361OlczKGh? MV\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;MD63NUDPxE1? M3z4eVIyPDZ|OUS0
human A2780 cells MX3GeY5kfGmxbjDhd5NigQ>? M4XmWVAvOjVizszN MmXWNlQhcA>? MoXGVoVlfWO2aX;uJIlvKE2lbEGgcIV3\WxiaX6gbJVu[W5iQUK3PFAh[2WubIOgZZQhOC5{NTD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MmTONlQ1PzF6N{O=

... 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 individually and in order:
water
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
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