Rigosertib (ON-01910)

目录号:S1362

Rigosertib (ON-01910) Chemical Structure

Molecular Weight(MW): 473.47

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。Phase 3。

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RMB 2630.22 现货
RMB 1381.36 现货
RMB 2625.85 现货
RMB 7944.48 现货
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客户使用该产品的4个实验数据:

  • (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.

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。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)
9 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 NVLRU3dnS3m2b4TvfIlkyqCjc4PhfS=> M3TWUVk3KGh? NYL4eY1WS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA6PiCqcoOgZpkhfHK7cHHuJIJtfWViZYjjcJV{cW:wIHHzd4F6NCCLQ{WwQVcvPSCwTR?= NEPGRW8zOThzMkSyNS=>
human T47D cells MoXDR5l1d3SxeHnjxsBie3OjeR?= MmrzO|IhcA>? M2\CfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHQ1P0RiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2xNEBvVQ>? NVy5[XNGOjF2NkO5OFQ>
human HeLa cells NVjaSI0xWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2[1VFczKGh? Mn\rRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0yOiCwTR?= NHj0bXQzPDR5MUi3Ny=>
human MDA468 cells MnrqR5l1d3SxeHnjxsBie3OjeR?= MVi3NkBp M1\Wc2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTR4ODDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVIxKG6P NXP2eYlCOjF2NkO5OFQ>
human LNCAP cells MlnOVJJwdGmoZYLheIlwdiCjc4PhfS=> MY[3NkBp M3jJN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRXIheG:|aYTpeoUhcHWvYX6gUG5ESVBiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUK1JI5O Moe1NlQ1PzF6N{O=
human PANC1 cells NX\FS3BLWHKxbHnm[ZJifGmxbjDhd5NigQ>? NV\5OXl5PzJiaB?= Ml;DRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQV7DNUBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFfJOVA:Ozlibl2= NIHFbVgzPDR5MUi3Ny=>
human MCF7 cells NHywco1Rem:uaX\ldoF1cW:wIHHzd4F6 MXm3NkBp M{XnR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSXIheG:|aYTpeoUhcHWvYX6gUWNHPyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NUCgcm0> NUPWOIhyOjR2N{G4O|M>
human HCT116 cells NXHvNopOS3m2b4TvfIlkyqCjc4PhfS=> MmjpO|IhcA>? M{e4ZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVUxKG6P MoG2NlE1PjN7NES=
human MCF7 cells M{nmTWN6fG:2b4jpZ:Kh[XO|YYm= NWT5T4Z1PzJiaB?= NUXwOpFES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVUxKG6P NYO4U3RuOjF2NkO5OFQ>
human MDA-MB-231 cells MkHlVJJwdGmoZYLheIlwdiCjc4PhfS=> M1ixOFczKGh? NWXPXnZwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBGWiCwZXfheIl3\SCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeR?= NXW4OG1OOjR2N{G4O|M>
human A2780 cells M4TwXHBzd2yrZnXyZZRqd25iYYPzZZk> M1vwTFczKGh? MkXpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFfJOVA:PjJibl2= MoHnNlQ1PzF6N{O=
human HCT116 cells M2\5bHBzd2yrZnXyZZRqd25iYYPzZZk> NYLBZmZUPzJiaB?= NX;HcY1TSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUewJI5O M1q4R|I1PDdzOEez
human DU145 cells M4nWOXBzd2yrZnXyZZRqd25iYYPzZZk> NXX4WVhEPzJiaB?= NV7PO3FSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBCWiCwZXfheIl3\SCqdX3hckBFXTF2NTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9O|Uhdk1? MXqyOFQ4OTh5Mx?=
human DU145 cells NX;DcWN1S3m2b4TvfIlkyqCjc4PhfS=> NUfsSXdjQTZiaB?= MmXaR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgPVYhcHK|IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCjc4PhfUwhUUN3ME23OUBvVQ>? MYGyNVgyOjR{MR?=
human MDA468 cells MmPqR5l1d3SxeHnjxsBie3OjeR?= MoD5OFghcA>? M3rwcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTR4ODDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVAvOzB{IN88US=> MkXPNlE1PjN7NES=
human MRC5 cells NGTvdmxEgXSxdH;4bYPDqGG|c3H5 MmPOO|IhcA>? NIXBcI5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9NE44OSEQvF2= NXHXe2o6OjF2NkO5OFQ>
human A2780 cells NX30c5IzTnWwY4Tpc44h[XO|YYm= M4PSOlAvOjVizszN NFHXOHEzPCCq NVvzfI9vWmWmdXP0bY9vKGmwIF3jcFEhdGW4ZXygbY4hcHWvYX6gRVI4QDBiY3XscJMh[XRiMD6yOUB2VSCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NXnkcZlNOjR2N{G4O|M>

... Click to View More Cell Line Experimental Data

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]
+ 展开

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]
+ 展开
  • 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]
+ 展开
  • Animal Models: 携带Bel-7402,MCF-7,和MIA-PaCa细胞的雌性无胸腺NCR-nu/nu鼠
  • Formulation: 溶于PBS
  • 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 从左到右依次加入纯溶剂:
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
稳定性 powder
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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 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