Rigosertib (ON-01910)

製品コードS1362

Rigosertib (ON-01910)化学構造

分子量(MW):473.47

Rigosertib (ON-01910)は一種の非ATP競争性的なPLK1阻害剤で、無細胞試験でIC50値が9 nMですが、PLK1に作用する選択性はPlk2に作用する選択性より30倍が高くなって、Plk3を抑制する活性がありません。臨床3期。

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カスタマーフィードバック(3)

  • 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.

製品安全説明書

PLK阻害剤の選択性比較

生物活性

製品説明 Rigosertib (ON-01910)は一種の非ATP競争性的なPLK1阻害剤で、無細胞試験でIC50値が9 nMですが、PLK1に作用する選択性はPlk2に作用する選択性より30倍が高くなって、Plk3を抑制する活性がありません。臨床3期。
靶点
PLK1 [1]
(Cell-free assay)
9 nM
In vitro試験

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 M4XnPGN6fG:2b4jpZ:Kh[XO|YYm= NEKwRnk6PiCq M37pOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCjc4PhfUwhUUN3ME23MlUhdk1? MlLhNlE5OTJ2MkG=
human T47D cells NHzqfoxEgXSxdH;4bYPDqGG|c3H5 MmjXO|IhcA>? MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;MUCgcm0> Mo\DNlE1PjN7NES=
human HeLa cells NVHNbmpEWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnzjO|IhcA>? M3LJZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXMZUBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFfJOVA:OTJibl2= MlTHNlQ1PzF6N{O=
human MDA468 cells MWfDfZRwfG:6aXRCpIF{e2G7 NHfaVY44OiCq NEfNdJJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEF2NkigZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0zOCCwTR?= M3HIWVIyPDZ|OUS0
human LNCAP cells MUnQdo9tcW[ncnH0bY9vKGG|c3H5 NVThZYRwPzJiaB?= MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFHSJJBwe2m2aY\lJIh2dWGwIFzOR2FRKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygS2k2OD1{NTDuUS=> NFHyW5ozPDR5MUi3Ny=>
human PANC1 cells Mo\VVJJwdGmoZYLheIlwdiCjc4PhfS=> MljLO|IhcA>? MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCDTlOxJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0{QSCwTR?= M4LQVFI1PDdzOEez
human MCF7 cells NITLSGFRem:uaX\ldoF1cW:wIHHzd4F6 MnjxO|IhcA>? MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFXSJJBwe2m2aY\lJIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTVyIH7N MYOyOFQ4OTh5Mx?=
human HCT116 cells NGDWe|lEgXSxdH;4bYPDqGG|c3H5 NFizZlM4OiCq M{LJNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVUxKG6P MnjyNlE1PjN7NES=
human MCF7 cells MVPDfZRwfG:6aXRCpIF{e2G7 M321eFczKGh? M{LlNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME21NEBvVQ>? MVeyNVQ3Ozl2NB?=
human MDA-MB-231 cells MmnXVJJwdGmoZYLheIlwdiCjc4PhfS=> MUG3NkBp MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFXSJI5m\2G2aY\lJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6 NYe5SllROjR2N{G4O|M>
human A2780 cells M{LuSnBzd2yrZnXyZZRqd25iYYPzZZk> NWHCfoFIPzJiaB?= NV3VVHVzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NkKgcm0> M1TQ[VI1PDdzOEez
human HCT116 cells NFO5cItRem:uaX\ldoF1cW:wIHHzd4F6 M1TWWFczKGh? MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFfJOVA:PzBibl2= M135fVI1PDdzOEez
human DU145 cells MUnQdo9tcW[ncnH0bY9vKGG|c3H5 NUXYN4JMPzJiaB?= MoLDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDBVkBv\WejdHn2[UBpfW2jbjDEWVE1PSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;N{Wgcm0> NVHpZ4pTOjR2N{G4O|M>
human DU145 cells NHvSfG5EgXSxdH;4bYPDqGG|c3H5 M3jRcVk3KGh? Ml;QR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgPVYhcHK|IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCjc4PhfUwhUUN3ME23OUBvVQ>? MkXSNlE5OTJ2MkG=
human MDA468 cells MYfDfZRwfG:6aXRCpIF{e2G7 MoX0OFghcA>? NXXvdmUzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDNE[4JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFfJOVA:OC5|MEKg{txO NWTBZ3k2OjF2NkO5OFQ>
human MRC5 cells NIOxPG5EgXSxdH;4bYPDqGG|c3H5 NG\URVQ4OiCq MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;MD63NUDPxE1? MoXpNlE1PjN7NES=
human A2780 cells MW\GeY5kfGmxbjDhd5NigQ>? MYCwMlI2KM7:TR?= M3T4flI1KGh? M{L3[nJm\HWldHnvckBqdiCPY3yxJIxmfmWuIHnuJIh2dWGwIFGyO|gxKGOnbHzzJIF1KDBwMkWgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? Mn6yNlQ1PzF6N{O=

... Click to View More Cell Line Experimental Data

In vivo試験 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]

プロトコル(参考用のみ)

キナーゼアッセイ:[1]
+ 展開

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.
細胞アッセイ: [2]
+ 展開
  • 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
    (参考用のみ)
動物実験:[1]
+ 展開
  • 動物モデル: Mouse (female athymic, NCR-nu/nu) xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells
  • 製剤: Dissolved in PBS
  • 投薬量: 250 mg/kg
  • 投与方法: Intraperitonially
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 95 mg/mL (200.64 mM)
Water 95 mg/mL (200.64 mM)
Ethanol <1 mg/mL
体内 water 95mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 473.47
化学式

C21H24NNaO8S

CAS No. 1225497-78-8
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID