|(2-甲氧基-5-(((2,4,6-三甲氧基苯乙烯基)磺酰基)甲基)苯基)甘氨酸钠盐|CsnPharm

CAS No.: 1225497-78-8

Sodium (2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)glycinate Catalog No. CSN15803

Synonyms: Rigosertib;ON-01910 Sodium(Random Configuration);ON-01910

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.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PLK1

IC50:9nM
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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1121 mL
- 10.5603 mL
- 21.1206 mL
- 5 mM
- 0.4224 mL
- 2.1121 mL
- 4.2241 mL
- 10 mM
- 0.2112 mL
- 1.0560 mL
- 2.1121 mL

技术信息

CAS号

1225497-78-8

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H24NNaO8S

运输

蓝冰

分子量

473.47

别名

Rigosertib;ON-01910 Sodium(Random Configuration);ON-01910;Rigosertib sodium;brand name: Estybon

溶解度

DMSO	550.0 mg/mL (1161.6 mM)
Water	90.0 mg/mL (190.1 mM) warming

动物实验配方

0.5% CMC-Na

40 mg/mL

suspension

大规格询价

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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

Sodium (2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)glycinate Catalog No. CSN15803

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