(E/Z)-Rigosertib sodium | (E/Z)-ON-01910 sodium;ON-01910 (sodium salt);ON-01910;Rigosertib | PLK

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(E/Z)-Rigosertib sodium 99%+

货号：A266562 同义名： (E/Z)-ON-01910 sodium;ON-01910 (sodium salt)

Rigosertib Sodium (Random Configuration) 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.

(E/Z)-Rigosertib sodium 化学结构
CAS号：1225497-78-8

(E/Z)-Rigosertib sodium 3D分子结构
CAS号：1225497-78-8

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(E/Z)-Rigosertib sodium 纯度/质量文件产品仅供科研

货号：A266562 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

PLK 亚型比较

产品名称	PLK1 ↓ ↑	PLK2 ↓ ↑	PLK3 ↓ ↑	PLK4 ↓ ↑	其他靶点	纯度
HMN-214	✔					99%+
SBE13 HCl	++++ PLK1, IC50: 200 pM					98%
Onvansertib	+++ PLK1, IC50: 2 nM					99%+
Volasertib	++++ PLK1, IC50: 0.87 nM					98%
GSK461364	+++ PLK1, Ki: 2.2 nM					99%+
MLN0905	+++ PLK1, IC50: 2 nM					99%+
Ro3280	++ PLK1, IC50: 3 nM					99%
(E/Z)-Rigosertib sodium	+ PLK1, IC50: 9 nM	+ PLK2, IC50: 260 nM			Bcr-Abl	99%+
BI 2536	++++ PLK1, IC50: 0.83 nM	++ PLK2, IC50: 3.5 nM	+ PLK3, IC50: 9.0 nM			99%+
CFI-400945				++ PLK4, IC50: 2.8 nM	Tie-2	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

(E/Z)-Rigosertib sodium 生物活性

靶点

PLK2

PLK2, IC50:260 nM
PLK1

PLK1, IC50:9 nM

描述

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. 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. 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.

(E/Z)-Rigosertib sodium 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human A2780 cells		Proliferation assay	72 h	Antiproliferative activity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50=62 nM	24471873
human A2780 cells	0.25 μM	Function assay	24 h	Reduction in Mcl1 level in human A2780 cells at 0.25 uM after 24 hrs by Western blot analysis	24471873
human DU145 cells		Proliferation assay	72 h	Antiproliferative activity against AR negative human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50=75 nM	24471873
human DU145 cells		Cytotoxic assay	96 h	Cytotoxicity against human DU145 cells after 96 hrs by trypan blue exclusion assay, IC50=75 nM	21812421

(E/Z)-Rigosertib sodium 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.56mL

2.11mL

1.06mL

21.12mL

4.22mL

2.11mL

(E/Z)-Rigosertib sodium 技术信息

CAS号	1225497-78-8
分子式	C₂₁H₂₄NNaO₈S
分子量	473.472

别名	(E/Z)-ON-01910 sodium;ON-01910 (sodium salt);ON-01910;Rigosertib
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

动物实验配方

PO 0.5% CMC-Na 40 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

human A2780 cells		Proliferation assay	72 h	Antiproliferative activity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50=62 nM	24471873
human A2780 cells	0.25 μM	Function assay	24 h	Reduction in Mcl1 level in human A2780 cells at 0.25 uM after 24 hrs by Western blot analysis	24471873
human DU145 cells		Proliferation assay	72 h	Antiproliferative activity against AR negative human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50=75 nM	24471873
human DU145 cells		Cytotoxic assay	96 h	Cytotoxicity against human DU145 cells after 96 hrs by trypan blue exclusion assay, IC50=75 nM	21812421
human HCT116 cells		Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, GI50=50 nM	21463944
human HCT116 cells		Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50=70 nM	24471873
human HeLa cells		Proliferation assay	72 h	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50=12 nM	24471873
human K562 cells		Cytotoxic assay	96 h	Cytotoxicity against human K562 cells after 96 hrs by trypan blue exclusion assay, IC50=7.5 nM	21812421
human LNCAP cells		Proliferation assay	72 h	Antiproliferative activity against AR positive human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50=25 nM	24471873
human MCF7 cells		Proliferation assay	72 h	Antiproliferative activity against ER positive human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50=50 nM	24471873
human MCF7 cells		Cytotoxic assay	72 h	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, GI50=50 nM	21463944
human MDA468 cells		Cytotoxic assay	72 h	Cytotoxicity against human MDA468 cells after 72 hrs by MTT assay, GI50=20 nM	21463944
human MDA468 cells		Cytotoxic assay	48 h	Cytotoxicity against human MDA468 cells after 48 hrs by MTT assay, GI50=0.302 μM	21463944
human MDA-MB-231 cells		Proliferation assay	72 h	Antiproliferative activity against ER negative human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay	24471873
human MRC5 cells		Cytotoxic assay	72 h	Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, GI50=0.71 μM	21463944
human PANC1 cells		Proliferation assay	72 h	Antiproliferative activity against human PANC1 cells assessed as cell growth inhibition after 72 hrs by MTT assay, GI50=39 nM	24471873
human T47D cells		Cytotoxic assay	72 h	Cytotoxicity against human T47D cells after 72 hrs by MTT assay, GI50=10 nM	21463944

(E/Z)-Rigosertib sodium 99%+

(E/Z)-Rigosertib sodium 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

(E/Z)-Rigosertib sodium 质控信息

(E/Z)-Rigosertib sodium 生物活性

(E/Z)-Rigosertib sodium 细胞研究

(E/Z)-Rigosertib sodium 实验方案

(E/Z)-Rigosertib sodium 技术信息

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(E/Z)-Rigosertib sodium 99%+

(E/Z)-Rigosertib sodium 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

(E/Z)-Rigosertib sodium 质控信息

(E/Z)-Rigosertib sodium 生物活性

(E/Z)-Rigosertib sodium 细胞研究

(E/Z)-Rigosertib sodium 实验方案

(E/Z)-Rigosertib sodium 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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