Rigosertib (ON-01910)

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. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.

Rigosertib (ON-01910)化学構造

CAS No. 1225497-78-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 55100 国内在庫あり
JPY 30200 国内在庫あり
JPY 55100 国内在庫あり
JPY 163000 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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製品安全説明書

現在のバッチを見る: 純度: 99.52%
99.52

Rigosertib (ON-01910)関連製品

シグナル伝達経路

PLK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
A2780 Function assay 0.25 uM 24 hrs Reduction in CDC25C level in human A2780 cells at 0.25 uM after 24 hrs by Western blot analysis 24471873
A2780 Apoptosis assay 0.25 uM 24 hrs Induction of apoptosis in human A2780 cells assessed as caspase-3/7 activation at 0.25 uM after 24 hrs by using Apo-ONE homogeneous caspase-3/7 kit 24471873
A2780 Function assay 0.25 uM 24 hrs Reduction in Mcl1 level in human A2780 cells at 0.25 uM after 24 hrs by Western blot analysis 24471873
MRC5 Function assay 1 uM Metabolic stability of the compound in human MRC5 cells at 1 uM 21463944
MCF7 Function assay 1 uM Metabolic stability of the compound in human MCF7 cells at 1 uM 21463944
LNCAP Antiproliferative assay 72 hrs Antiproliferative activity against AR positive human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.025 μM. 24471873
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.012 μM. 24471873
DU145 Cytotoxicity assay 96 hrs Cytotoxicity against human DU145 cells after 96 hrs by trypan blue exclusion assay, IC50 = 0.075 μM. 21812421
K562 Cytotoxicity assay 96 hrs Cytotoxicity against human K562 cells after 96 hrs by trypan blue exclusion assay, IC50 = 0.0075 μM. 21812421
MRC5 Cytotoxicity assay 72 hrs Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, GI50 = 0.71 μM. 21463944
MDA468 Cytotoxicity assay 24 hrs Cytotoxicity against human MDA468 cells after 24 hrs by MTT assay, GI50 = 0.601 μM. 21463944
MDA468 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA468 cells after 48 hrs by MTT assay, GI50 = 0.302 μM. 21463944
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, GI50 = 0.05 μM. 21463944
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, GI50 = 0.05 μM. 21463944
MDA468 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA468 cells after 72 hrs by MTT assay, GI50 = 0.02 μM. 21463944
T47D Cytotoxicity assay 72 hrs Cytotoxicity against human T47D cells after 72 hrs by MTT assay, GI50 = 0.01 μM. 21463944
PANC1 Antiproliferative assay 72 hrs Antiproliferative activity against human PANC1 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.039 μM. 24471873
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against ER positive human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.05 μM. 24471873
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.05 μM. 24471873
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against ER negative human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.057 μM. 24471873
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.062 μM. 24471873
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.07 μM. 24471873
DU145 Antiproliferative assay 72 hrs Antiproliferative activity against AR negative human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50 = 0.075 μM. 24471873
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生物活性

製品説明 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. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. 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)
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9 nM 18 nM 32 nM 42 nM 155 nM
In Vitro
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]
Kinase Assay 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.
細胞実験 細胞株 A number of tumor cell lines, including BT20, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, HeLa, and Raji cells
濃度 1 nM - 10 μM, dissolved in DMSO as stock solution.
反応時間 96 hours
実験の流れ 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
実験結果図 Methods Biomarkers 結果図 PMID
Western blot pAbl / Abl / PCrk-L / Crk-L / Cleaved caspase3 / Cleaved PARP / pHistone H2A.X 26008977
Immunofluorescence p-ATF / COX IV 27764820
Growth inhibition assay GI50 Cell viability 29108241
In Vivo
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]
動物実験 動物モデル Mouse (female athymic, NCR-nu/nu) xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells
投与量 250 mg/kg
投与経路 Intraperitonially
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04177498 Recruiting
Recessive Dystrophic Epidermolysis Bullosa
Thomas Jefferson University|Onconova Therapeutics Inc.
August 24 2021 Early Phase 1
NCT02075034 Withdrawn
Myelodysplastic Syndrome
Onconova Therapeutics Inc.
May 2014 Phase 1
NCT02030639 Completed
Healthy
Onconova Therapeutics Inc.
January 2014 Phase 1
NCT01928537 Completed
Myelodysplastic Syndromes|Refractory Anemia With Excess Blasts|Chronic Myelomonocytic Leukemia|Cytopenia
Onconova Therapeutics Inc.
August 2013 Phase 3
NCT01807546 Completed
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
Solid Tumor
Onconova Therapeutics Inc.
July 2010 Phase 1

化学情報

分子量 473.47 化学式

C21H24NNaO8S

CAS No. 1225497-78-8 SDF Download Rigosertib (ON-01910) SDFをダウンロードする
Smiles COC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)[O-].[Na+]
保管

In vitro
Batch:

DMSO : 94 mg/mL ( (198.53 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 94 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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