1225497-78-8

1225497-78-8 - Names and Identifiers

Name	sodium (E)-2-((2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)amino)acetate
Synonyms	Estybon ESTYBON ON-01910 ON 01910 sodium salt Rigosertib (ON-01910) sodium (E)-2-((2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)amino)acetate N-[2-Methoxy-5-[[[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]glycine sodium salt N-[2-Methoxy-5-[[[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]glycine sodium salt Rigosertib (ON-01910)
CAS	1225497-78-8

1225497-78-8 - Physico-chemical Properties

Molecular Formula	C21H24NNaO8S
Molar Mass	473.47193
Melting Point	>256oC (dec.)
Solubility	DMSO: 50 mg/mL mother liquor preservation: sub-package and freeze storage to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, try to use it now) Cell experiment: Dissolve with DMSO first: dilute with culture medium then, and the dilution process is recommended to be carried out in stages to avoid too fast concentration change leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to avoid excessive concentration changes leading to compound pr
Appearance	Solid
Color	Pale Yellow to Pale Green
Storage Condition	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
Use	Rigosertib (ON-01910 sodium salt) is a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity. Polo-like kinase 1 inhibitor ON 01910.Na inhibits polo-like kinase1 (Plk1), inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. This agent may exhibit synergistic antitumor activity in combination with other chemotherapeutic agents. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner. Note: this product is supplied as sodium salt.
Target	PLK1
In vitro study	Rigosertib is a non-ATP competitive inhibitor of PLK1 with an IC50 of 9 nM. Rigosertib also inhibited PLK2,PDGFR,Flt1,BCR-ABL,Fyn,Src and CDK1 with an IC50 of 18-260 nM. Rigosertib has Cell Death activity, acting on 94 different tumor cell lines, IC50 is 50-250 nM, including BT27,MCF-7,DU145,PC3,U87,A549,H187,RF1,HCT15,SW480, and KB cells. Rigosertib has no effect on normal cells, such as HFL, Proc, HMEC, and HUVEC, unless the concentration of action is higher than 5-10 μm. 100-250 nM Rigosertib acts on HeLa cells to induce spindle variation and apoptosis. Rigosertib also inhibits a number of multidrug-resistant tumor cell lines, including MES-SA, MES-SA/DX5a, CEM, and CEM/C2a, with an IC50 of 50-nM. 0.25-5 µm Rigosertib acts on DU145 cells, inhibits the cell cycle, stops the cells in G2/M phase, and activates the apoptotic pathway. 50 nM-0.5 µm Rigosertib acts on A549 cells, inducing loss of viability and caspase 3/7 activation. Recent studies have shown that Rigosertib acts on chronic lymphocytic leukemia (CLL) cells, inducing apoptosis, and has no toxicity on T cells or normal B cells. Rigosertib chronic lymphocytic leukemia (CLL) cells also inhibit the pro-survival effect of follicular dendritic cells, acting on leukemia cells, reducing SDF-1 induced migration.
In vivo study	Rigosertib at a dose of 250 mg/kg significantly inhibited tumor growth in murine xenograft tumor models carrying Bel-7402,MCF-7, and MIA-PaCa cells. Rigosertib also inhibited tumor growth at a dose of 200 mg/kg in a murine transplanted tumor model carrying BT20 cells.

1225497-78-8 - Reference

Reference

1: Lucas CD, Dorward DA, Tait MA, Fox S, Marwick JA, Allen KC, Robb CT, Hirani N, Haslett C, Duffin R, Rossi AG. Downregulation of Mcl-1 has anti-inflammatory pro-resolution effects and enhances bacterial clearance from the lung. Mucosal Immunol. 2013 Nov 27. doi: 10.1038/mi.2013.102. [Epub ahead of print] PubMed PMID: 24280938.
2: Dolman ME, den Hartog IJ, Molenaar JJ, Schellens JH, Beijnen JH, Sparidans RW. Liquid chromatography-tandem mass spectrometric assay for the cyclin-dependent kinase inhibitor AT7519 in mouse plasma. J Pharm Biomed Anal. 2014 Jan 25;88:216-20. doi: 10.1016/j.jpba.2013.08.051. Epub 2013 Sep 12. PubMed PMID: 24080524.
3: Alessandri AL, Duffin R, Leitch AE, Lucas CD, Sheldrake TA, Dorward DA, Hirani N, Pinho V, de Sousa LP, Teixeira MM, Lyons JF, Haslett C, Rossi AG. Induction of eosinophil apoptosis by the cyclin-dependent kinase inhibitor AT7519 promotes the resolution of eosinophil-dominant allergic inflammation. PLoS One. 2011;6(9):e25683. doi: 10.1371/journal.pone.0025683. Epub 2011 Sep 30. PubMed PMID: 21984938; PubMed Central PMCID: PMC3184151.
4: Mahadevan D, Plummer R, Squires MS, Rensvold D, Kurtin S, Pretzinger C, Dragovich T, Adams J, Lock V, Smith DM, Von Hoff D, Calvert H. A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors. Ann Oncol. 2011 Sep;22(9):2137-43. doi: 10.1093/annonc/mdq734. Epub 2011 Feb 16. PubMed PMID: 21325451.
5: Squires MS, Cooke L, Lock V, Qi W,

1225497-78-8 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	2.112 ml	10.56 ml	21.121 ml
5 mM	0.422 ml	2.112 ml	4.224 ml
10 mM	0.211 ml	1.056 ml	2.112 ml
5 mM	0.042 ml	0.211 ml	0.422 ml

Last Update：2024-01-02 23:10:35

1225497-78-8 - Cell Experiment

Cells are grown in either DMEM or RPMI supplemented with 10% fetal bovine serum and 1 unit/mL penicillin-streptomycin solution. Tumor cells are plated into six-well dishes at a density of 1 × 105cells/mL/well, and Rigosertib is added 24 hours later at various concentrations. Cell counts are determined from duplicate wells after 96-hour of treatment. The total number of viable cells is determined by trypan blue exclusio(Only for Reference) Cell lines: A number of tumor cell lines, including BT20, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, HeLa, and Raji cells

Last Update：2023-08-16 21:32:38