计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
ON-01910是PLK1的抑制剂，IC50为9 nM。ON-01910还抑制PLK2，PDGFR，Flt1，BCR-ABL，Fyn，Src和CDK1，IC50为18–260 nM。ON-01910显示了对94种不同肿瘤细胞系的杀伤活性，IC50为50–250 nM，包括BT27，MCF-7，DU145，PC3，U87，A549，H187，RF1，HCT15，SW480和KB细胞。在HeLa细胞中，ON-01910（100–250 nM）会诱导纺锤体异常和凋亡。ON-01910还抑制几种多药耐药肿瘤细胞系
Information
Rigosertib (ON-01910) is a non-ATP-competitive inhibitor ofPLK1withIC50of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibitsPI3K/Aktpathway and activates oxidative stress signals. Rigo
In vitro
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.
In vivo
In mouse xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells, Rigosertib (250 mg/kg) markedly inhibits tumor growth. Rigosertib (200 mg/kg) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells.
Cell Data
cell lines：
Concentrations：1 nM - 10 μM, dissolved in DMSO as stock solution.
Incubation Time：96 hours
Powder Purity:≥98%
规格
英文别名
N-[2-methoxy-5-[[[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]-glycine,sodium salt (1:1)
规格或纯度
10mM in DMSO
英文名称
Rigosertib (ON-01910)
生化机理
Rigosertib（ON-01910）是一种非ATP竞争性 PLK1 抑制剂，在无细胞试验中的 IC50 为 9 nM。它对 Plk2 的选择性高出 30 倍，对 Plk3 没有活性。Rigosertib 可抑制 PI3K/Akt 通路并激活氧化应激信号。Rigosertib 可诱导多种癌细胞凋亡。第 3 阶段
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=C(C=C(C=C1)CS(=O)(=O)/C=C/C2=C(C=C(C=C2OC)OC)OC)NCC(=O)[O-].[Na+]
分子量
473.43
Reaxy-Rn
26934487
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26934487&ln=
技术文档
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 48 mg/mL (198.91 mM);
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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