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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Cited by 19 Publications

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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 NWfweoF6S3m2b4TvfIlkyqCjc4PhfS=> NUmxTWVHQTZiaB?= NHm1S3JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFk3KGi{czDifUB1enmyYX6gZox2\SCneHPseZNqd25iYYPzZZktKEmFNUC9O{42KG6P MlrXNlE5OTJ2MkG=
human T47D cells NG\zPHlEgXSxdH;4bYPDqGG|c3H5 MUi3NkBp NFjpV4tEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVPDeGIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9NVAhdk1? NGrNb48zOTR4M{m0OC=>
human HeLa cells MljzVJJwdGmoZYLheIlwdiCjc4PhfS=> MnTlO|IhcA>? NHXFdWpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTF{IH7N MXKyOFQ4OTh5Mx?=
human MDA468 cells MXzDfZRwfG:6aXRCpIF{e2G7 NV;yTms1PzJiaB?= MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGE1PjhiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2yNEBvVQ>? M2LrfVIyPDZ|OUS0
human LNCAP cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 NUDE[4wzPzJiaB?= MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFHSJJBwe2m2aY\lJIh2dWGwIFzOR2FRKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygS2k2OD1{NTDuUS=> NFTCWYkzPDR5MUi3Ny=>
human PANC1 cells MkDhVJJwdGmoZYLheIlwdiCjc4PhfS=> NUTubFc2PzJiaB?= NVTDR3g1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQRW5EOSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;M{mgcm0> NUezZZlvOjR2N{G4O|M>
human MCF7 cells M2jaVHBzd2yrZnXyZZRqd25iYYPzZZk> M2DlTFczKGh? MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFXSJJBwe2m2aY\lJIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTVyIH7N MlLJNlQ1PzF6N{O=
human HCT116 cells MoDQR5l1d3SxeHnjxsBie3OjeR?= NYfhO5lLPzJiaB?= MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME21NEBvVQ>? NWey[pdPOjF2NkO5OFQ>
human MCF7 cells MnXUR5l1d3SxeHnjxsBie3OjeR?= M1vtRlczKGh? MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NUCgcm0> NWi4[HBiOjF2NkO5OFQ>
human MDA-MB-231 cells NYTJe2ZOWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlfyO|IhcA>? Ml\JRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDFVkBv\WejdHn2[UBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigQ>? M3LLbVI1PDdzOEez
human A2780 cells MorjVJJwdGmoZYLheIlwdiCjc4PhfS=> NIPVbok4OiCq M2TrT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTZ{IH7N NH\IZYUzPDR5MUi3Ny=>
human HCT116 cells MYXQdo9tcW[ncnH0bY9vKGG|c3H5 M4LHdVczKGh? MmPBRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTdyIH7N MnXJNlQ1PzF6N{O=
human DU145 cells NYrsU4U1WHKxbHnm[ZJifGmxbjDhd5NigQ>? MYq3NkBp MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFHSJI5m\2G2aY\lJIh2dWGwIFTVNVQ2KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygS2k2OD15NTDuUS=> M2PPUFI1PDdzOEez
human DU145 cells Ml\HR5l1d3SxeHnjxsBie3OjeR?= MYO5OkBp NF\IR5ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCjZoTldkA6PiCqcoOgZpkhfHK7cHHuJIJtfWViZYjjcJV{cW:wIHHzd4F6NCCLQ{WwQVc2KG6P MorBNlE5OTJ2MkG=
human MDA468 cells MXPDfZRwfG:6aXRCpIF{e2G7 MlSxOFghcA>? NYO3NmM1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDNE[4JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFfJOVA:OC5|MEKg{txO MYqyNVQ3Ozl2NB?=
human MRC5 cells MVLDfZRwfG:6aXRCpIF{e2G7 NXPCN2U2PzJiaB?= MoXSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUCuO|Eh|ryP M2LkTVIyPDZ|OUS0
human A2780 cells NHjoOmJHfW6ldHnvckBie3OjeR?= MUSwMlI2KM7:TR?= M37GS|I1KGh? NGfoWVlT\WS3Y4Tpc44hcW5iTXPsNUBt\X[nbDDpckBpfW2jbjDBNlc5OCClZXzsd{BifCByLkK1JJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MlHwNlQ1PzF6N{O=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pAbl / Abl / PCrk-L / Crk-L / Cleaved caspase3 / Cleaved PARP / pHistone H2A.X; 

PubMed: 26008977     


Ba/F3 T315I cells were treated with rigosertib at the indicated concentrations for 24 h. Total extracts were examined via immunoblotting with anti-phospho ABL, phospho-Crk-L, phosphohistone H2A.X, cleaved caspase 3, cleaved-PARP, ABL, Crk-L, and β-actin antibodies (abs). ABL, Abelson; PARP, poly (ADP-ribose) polymerase; abs, antibodies.

26008977
Immunofluorescence
p-ATF / COX IV; 

PubMed: 27764820     


Representative confocal microscopy images of FaDu, UMSCC 47 and D-HMVEC cells treated with rigosertib (1.0 μM) or ON 01911.Na (1.0 μM) for 24 h before fixing, staining with indicated antibodies, and capturing images. Green: p-ATF; Red: Cox IV (mitochondrial marker); Blue: DAPI (nuclear marker).

27764820
Growth inhibition assay
GI50; 

PubMed: 29108241     


The GI50 values of BI2536, rigosertib, and poloxin were determined in both parental and volasertib-resistant R-MOLM14 and R-HL-60. Error bars represent the mean values ± S.D. of at least three independent experiments.

Cell viability; 

PubMed: 27764820     


Cell viability as measured by MTS. FaDu, Detroit 562, UMSCC 1, UMSCC 47 and UMSCC 104 cells were treated with increasing concentrations of rigosertib for 48 h, and cell viability was assessed. 50% growth inhibition (IC50) is recorded for each cell line in μM in the legend. Untreated cells were considered 100% viable and percent viability of cells treated with rigosertib was calculated vs. this control. Data represent the mean +/− SD of 3 independent experiments.

29108241 27764820
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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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(Data is from Selleck tests instead of citations):
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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02075034 Suspended Drug: rigosertib Myelodysplastic Syndrome Onconova Therapeutics Inc. May 2014 Phase 1
NCT02030639 Completed Drug: rigosertib Healthy Onconova Therapeutics Inc. January 2014 Phase 1
NCT01928537 Active not recruiting Drug: rigosertib sodium Myelodysplastic Syndromes|Refractory Anemia With Excess Blasts|Chronic Myelomonocytic Leukemia|Cytopenia Onconova Therapeutics Inc. August 2013 Phase 3
NCT01807546 Completed Drug: rigosertib Head and Neck Squamous Cell Carcinoma|Anal Squamous Cell Carcinoma|Lung Squamous Cell Carcinoma|Cervical Squamous Cell Carcinoma|Esophageal Squamous Cell Carcinoma|Skin Squamous Cell Carcinoma|Penile Squamous Cell Carcinoma Onconova Therapeutics Inc. March 2013 Phase 2
NCT01168011 Completed Drug: rigosertib Solid Tumor Onconova Therapeutics Inc. July 2010 Phase 1
NCT01167166 Completed Drug: rigosertib Acute Myelocytic Leukemia|Acute Lymphocytic Leukemia|Myeloproliferative Disease|Chronic Myeloid Leukemia Onconova Therapeutics Inc. July 2010 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID