Rigosertib (ON-01910)

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。

Rigosertib (ON-01910) Chemical Structure

Rigosertib (ON-01910) Chemical Structure

CAS: 1225497-78-8

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2630.22 现货
5mg RMB 1381.36 现货
50mg RMB 7944.48 现货
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客户使用Selleck的Rigosertib (ON-01910)发表文献32

产品质控

批次: 纯度: 99.28%
98.01

Rigosertib (ON-01910)相关产品

相关信号通路图

PLK抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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

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)
点击更多
9 nM 18 nM 32 nM 42 nM 155 nM
体外研究(In Vitro)
体外研究活性 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]
激酶实验 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 细胞系 多种肿瘤细胞系,包括 BT20,MCF-7,DU145,PC3,U87,A549,H187,RF1,HCT15,HeLa,和Raji细胞
浓度 1 nM-10 µM, 溶于DMSO,作为储存液
孵育时间 96小时
方法 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。
实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性 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]
动物实验 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
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

化学信息&溶解度

分子量 473.47 分子式

C21H24NNaO8S

CAS号 1225497-78-8 SDF Download Rigosertib (ON-01910) SDF
Smiles COC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)[O-].[Na+]
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 95 mg/mL ( 200.64 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : 95 mg/mL

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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