Rigosertib (ON-01910)

For research use only. Not for use in humans.

目录号:S1362

Rigosertib (ON-01910) Chemical Structure

CAS No. 1225497-78-8

Rigosertib (ON-01910) 是一种非ATP竞争性PLK1抑制剂,无细胞试验中IC50为9 nM,比作用于Plk2选择性高30倍,对Plk3没有抑制活性。Rigosertib 可抑制 PI3K/Akt 信号通路并激活氧化应激信号。Rigosertib 可诱导多种癌细胞的凋亡。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2630.22 现货
RMB 1381.36 现货
RMB 2625.85 现货
RMB 7944.48 现货
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客户使用Selleck生产的Rigosertib (ON-01910)发表文献24篇:

产品安全说明书

PLK抑制剂选择性比较

生物活性

产品描述 Rigosertib (ON-01910) 是一种非ATP竞争性PLK1抑制剂,无细胞试验中IC50为9 nM,比作用于Plk2选择性高30倍,对Plk3没有抑制活性。Rigosertib 可抑制 PI3K/Akt 信号通路并激活氧化应激信号。Rigosertib 可诱导多种癌细胞的凋亡。Phase 3。
特性 Rigosertib是作用于Polo样激酶(PLK1)的非ATP竞争性抑制剂。
靶点
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
体外研究

Rigosertib是PLK1的非ATP竞争性抑制剂,IC50为9 nM。Rigosertib也抑制 PLK2,PDGFR,Flt1,BCR-ABL,Fyn,Src和CDK1, IC50为18-260 nM。Rigosertib具有使细胞死亡的活性,作用于94种不同肿瘤细胞系,IC50为50-250 nM,包括BT27,MCF-7,DU145,PC3,U87,A549,H187,RF1,HCT15,SW480,和KB细胞。Rigosertib作用于正常细胞,如 HFL,PrEC,HMEC,和HUVEC没有效果,除非作用浓度高于5-10 µM。100-250 nM Rigosertib作用于HeLa 细胞,诱导纺锤体变异和凋亡。[1] Rigosertib也抑制一些多重耐药的的肿瘤细胞系,包括 MES-SA, MES-SA/DX5a, CEM, 和 CEM/C2a, IC50为50-100 nM。0.25-5 µM Rigosertib作用于DU145细胞, 抑制细胞周期,使细胞停在G2/M 期,和激活凋亡通路。50 nM-0.5 µM Rigosertib作用于A549细胞,诱导存活力和caspase 3/7激活的丧失。[2]最新研究显示, Rigosertib作用于慢性淋巴细胞性白血病 (CLL)细胞,诱导凋亡,且作用于T细胞或正常B细胞没有毒性。Rigosertib 慢性淋巴细胞性白血病(CLL)细胞,也抑制滤泡树突状细胞的促生存效果,作用于白血病细胞,降低SDF-1诱导的迁移 。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human K562 cells M1O0emN6fG:2b4jpZ:Kh[XO|YYm= Mo\4PVYhcA>? MoXaR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC5OkBpenNiYomgeJJ6eGGwIHLseYUh\XilbIXzbY9vKGG|c3H5MEBKSzVyPUeuOUBvVQ>? Mn\yNlE5OTJ2MkG=
human T47D cells NFPmTYhEgXSxdH;4bYPDqGG|c3H5 NWSze|NWPzJiaB?= MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;MUCgcm0> M4PSXlIyPDZ|OUS0
human HeLa cells NYn5O|ExWHKxbHnm[ZJifGmxbjDhd5NigQ>? MorIO|IhcA>? MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVEzKG6P MUeyOFQ4OTh5Mx?=
human MDA468 cells NIS4R|lEgXSxdH;4bYPDqGG|c3H5 M2\mVVczKGh? MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGE1PjhiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2yNEBvVQ>? NHHQXm0zOTR4M{m0OC=>
human LNCAP cells M3TUXnBzd2yrZnXyZZRqd25iYYPzZZk> NHXsPZM4OiCq NUjmTVBGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBCWiCyb4PpeIl3\SCqdX3hckBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9NlUhdk1? NVrLZpZvOjR2N{G4O|M>
human PANC1 cells MoLrVJJwdGmoZYLheIlwdiCjc4PhfS=> M3zuPFczKGh? M33IV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFHOR|Eh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTN7IH7N MUCyOFQ4OTh5Mx?=
human MCF7 cells NEDYb3pRem:uaX\ldoF1cW:wIHHzd4F6 MYG3NkBp NVTuTWpCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBGWiCyb4PpeIl3\SCqdX3hckBOS0Z5IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME21NEBvVQ>? NUjmXopWOjR2N{G4O|M>
human HCT116 cells M374OGN6fG:2b4jpZ:Kh[XO|YYm= M4\GZ|czKGh? MnK3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9OVAhdk1? MoKyNlE1PjN7NES=
human MCF7 cells NYrSU2wzS3m2b4TvfIlkyqCjc4PhfS=> M3zwblczKGh? MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NUCgcm0> NUXPXpRiOjF2NkO5OFQ>
human MDA-MB-231 cells MnPXVJJwdGmoZYLheIlwdiCjc4PhfS=> M{jKVVczKGh? MkHWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDFVkBv\WejdHn2[UBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigQ>? MlX1NlQ1PzF6N{O=
human A2780 cells NHzISYJRem:uaX\ldoF1cW:wIHHzd4F6 NGHpbZc4OiCq NFvtN3dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygS2k2OD14MjDuUS=> NWnlVmZEOjR2N{G4O|M>
human HCT116 cells MlnVVJJwdGmoZYLheIlwdiCjc4PhfS=> M1vDflczKGh? NUO2Z2s5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUewJI5O NVm2fmZQOjR2N{G4O|M>
human DU145 cells M{jhfXBzd2yrZnXyZZRqd25iYYPzZZk> M13m[lczKGh? M1W0VmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRXIhdmWpYYTpeoUhcHWvYX6gSHUyPDViY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUe1JI5O MWGyOFQ4OTh5Mx?=
human DU145 cells MmLGR5l1d3SxeHnjxsBie3OjeR?= NYXuclJLQTZiaB?= M13MSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGGodHXyJFk3KGi{czDifUB1enmyYX6gZox2\SCneHPseZNqd25iYYPzZZktKEmFNUC9O|Uhdk1? NYLXdnZsOjF6MUK0NlE>
human MDA468 cells MoPCR5l1d3SxeHnjxsBie3OjeR?= M{DyPFQ5KGh? MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGE1PjhiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2wMlMxOiEQvF2= MV2yNVQ3Ozl2NB?=
human MRC5 cells NYXkU4o5S3m2b4TvfIlkyqCjc4PhfS=> M4LIOVczKGh? NWPNPG11S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVKFNTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVAvPzFizszN M1u4bFIyPDZ|OUS0
human A2780 cells NHT6[|RHfW6ldHnvckBie3OjeR?= NEnVb48xNjJ3IN88US=> MkW4NlQhcA>? MoHEVoVlfWO2aX;uJIlvKE2lbEGgcIV3\WxiaX6gbJVu[W5iQUK3PFAh[2WubIOgZZQhOC5{NTD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NUnaZ2k2OjR2N{G4O|M>

... 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
体内研究 Rigosertib按250 mg/kg剂量作用于携带Bel-7402,MCF-7,和MIA-PaCa细胞的鼠移植瘤模型,明显抑制肿瘤生长。[1]Rigosertib按200 mg/kg剂量作用于携带BT20细胞的鼠移植瘤模型,也抑制肿瘤生长。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

体外测定PLK1的酶实验:

10 ng 重组PLK1和不同浓度Rigosertib在15 µL反应混合物(50 mM HEPES,10 mM MgCl2,1 mM EDTA,2 mM二硫苏糖醇,0.01% NP-40,pH 为7.5)中在室温下反应30分钟。激酶反应在20 µL反应混合物[15 µL 酶 + 抑制剂, 2 µL 1 mM ATP, 2 µL γ32P ATP (40 μci), 和1 µL 重组Cdc25C (100 ng)或酪蛋白 (1 μg) 底物]在30oC下进行20分钟。在20 µL 2× Laemmli buffer中沸腾2分钟终止反应。通过18% SDS-PAGE分离磷酸化的底物。烘干凝胶柱,用X-射线处理3-10分钟。
细胞实验:[2]
- 合并
  • Cell lines: 多种肿瘤细胞系,包括 BT20,MCF-7,DU145,PC3,U87,A549,H187,RF1,HCT15,HeLa,和Raji细胞
  • Concentrations: 1 nM-10 µM, 溶于DMSO,作为储存液
  • Incubation Time: 96小时
  • Method: 细胞生长在含10%FBS和1 unit/mL青霉素-链霉亲和素溶液的DMEM或RPMI培养基中。肿瘤细胞按每孔1×105个细胞接种在6孔板上,24小时后,加入不同浓度Rigosertib。处理96小时后,测定每孔细胞数。通过台酚蓝染色测定全部存活细胞数。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 携带Bel-7402,MCF-7,和MIA-PaCa细胞的雌性无胸腺NCR-nu/nu鼠
  • Dosages: 250 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 95 mg/mL (200.64 mM)
Water 95 mg/mL (200.64 mM)
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
water
95mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 473.47
化学式

C21H24NNaO8S

CAS号 1225497-78-8
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04177498 Not yet recruiting Drug: Rigosertib Sodium|Other: Quality-of-Life Assessment Recessive Dystrophic Epidermolysis Bullosa Thomas Jefferson University|Onconova Therapeutics Inc. September 1 2020 Early Phase 1
NCT02075034 Withdrawn Drug: rigosertib Myelodysplastic Syndrome Onconova Therapeutics Inc. May 2014 Phase 1
NCT02030639 Completed Drug: rigosertib Healthy Onconova Therapeutics Inc. January 2014 Phase 1
NCT01928537 Completed 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID