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Rigosertib sodium

  Cat. No.:  DC24085   Featured
Chemical Structure
592542-60-4
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More than 5000 active chemicals with high quality for research!
Field of application
Rigosertib sodium (ON 01910.Na) is a potent, non-ATP-competitive PLK1 inhibitor (IC50=9-10 nM), selectively induces mitotic G2/M arrest and apoptosis in cancer cells.
Cas No.: 592542-60-4
Chemical Name: Rigosertib sodium
Synonyms: Glycine, N-[2-methoxy-5-[[[(1E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]-, sodium Slat;RIGOSERTIB SODIUM;Sodium {[2-methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)vinyl]sulfo nyl}methyl)phenyl]amino}acetate;ON01910 sodium;ON-01910 sodium;(E)-2,4,6-Trimethoxystyryl 3-[(carboxymethyl)amino]-4-methoxybenzyl sulfone sodium salt;Novonex;ON 01910 sodium salt;Rigosertib (sodium);SCHEMBL498729;EX-A2149;GLYCINE, N-(2-METHOXY-5-((((1E)-2-(2,4,6-TRIMETHOXYPHENYL)ETHENYL)SULFONYL)METHYL)PHENYL)-, SODIUM SALT (1:1);Rigosertib sodium [USAN];1225497-78-8;SODIUM 2-[(2-METHOXY-5-{[2-(2,4,6-TRIMETHOXYPHENYL)ETHENESULFONYL]METHYL}PHENYL)AMINO]ACETATE;A11955;s1362;Glycine, N-[2-methoxy-5-[[[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]-, sodium salt (1:1);Q27258295;SW219255-1;Glycine, N-(2-methoxy-5-((((1E)-2-(2,4,6-trimethoxyphenyl)ethenyl)sulfonyl)methyl)phenyl)-, monosodium salt;ON-1910Na;Rigosertib; ON-01910;BR175409;sodium [2-methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)anilino]acetate;sodium (E)-(2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)glycinate;RIGOSERTIB SODIUM [WHO-DD];Rigosertib (ON-01910);ON-01910 sodium salt;Rigosertib Sodium(Random Configuration);406FL5G00V;Sodium (2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)glycinate;CHEMBL2013119;BCP08297;AS-74823;(E)-ON 01910.Na;(e)-2-(5-((2,4,6-trimethoxystyrylsulfonyl)methyl)-2-methoxyphenylamino)acetic acid sodium salt;UNII-406FL5G00V;rigosertib sodium salt;AKOS025404906;Sodium (E)-2-(2-methoxy-5-((2,4,6-trimethoxystyrylsulfonyl)methyl)phenylamino)acetate;DA-57444;Glycine, N-[2-Methoxy-5-[[[(1E)-2-(2,4,6-triMethoxyphenyl)ethenyl]sulfonyl]Methyl]phenyl]-, sodiuM Slat;ON-01910;Estybon;RIGOSERTIB SODIUM [JAN];VLQLUZFVFXYXQE-USRGLUTNSA-M;BCP02852;CS-0012458;EX-A4081;Rigosertib sodium;Estybon, ON-01910;Rigosertib?;BCP9001024;AC-32845;ON 01910 sodium;D10155;EX-8601;592542-60-4;HY-18651;RIGOSERTIB, ON-01910;ON 01910.Na;CCG-269479;sodium;2-[2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]anilino]acetate;SyB L-1101;Rigosertib sodium?;(E/Z)-Rigosertib (sodium);sodium (E)-2-((2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)amino)acetate;CHEBI:145421;AC-36514;Onc-01910;SyB C-1101;Rigosertib sodium (JAN/USAN);ON-01910.Na;ON-01910Na
SMILES: COC1=CC=C(C=C1NCC([O-])=O)CS(/C=C/C2=C(C=C(C=C2OC)OC)OC)(=O)=O.[Na+]
Formula: C21H24NO8S-.Na+
M.Wt: 473.47196
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Rigosertib (sodium) is a non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM, and shows 30-fold selectivity over PLK2.
Target: PLK1:9 nM (IC50) PLK2:260 nM (IC50) PDGFR:18 nM (IC50) Src:155 nM (IC50) BCR-ABL:32 nM (IC50) Cdk1:260 nM (IC50) Flt1:42 nM (IC50) Fyn:182 nM (IC50)
In Vivo: Rigosertib (250 mg/kg, i.p.) markedly inhibits tumor growth in mouse xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells[1]. Rigosertib (200 mg/kg, i.p.) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells[2].
In Vitro: Rigosertib is non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM. Rigosertib also exhibits inhibition of 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[1]. 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[2]. Rigosertib sodium (2 μM) induces apoptosis in chronic lymphocytic leukemia (CLL) cells without toxicity against T-cells or normal B-cells. Rigosertib sodium (2 μM) also abrogates the pro-survival effect of follicular dendritic cells on CLL cells and reduces SDF-1-induced migration of leukemic cells[3].
Kinase Assay: Recombinant PLK1 (10 ng) is incubated with different concentrations of Rigosertib in a 15 µL reaction mixture (50 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 2 mM Dithiothreitol, 0.01% NP-40 [pH 7.5]) for 30 min at room temperature. Kinase reactions are performed for 20 min at 30°C in a volume of 20 µL (15 µL enzyme + inhibitor, 2 µL 1 mM ATP), 2 µL of γ32P-ATP (40 μCi), and 1 µL of recombinant Cdc25C (100 ng) or casein (1 μg) substrates. Reactions are terminated by boiling for 2 min in 20 µL of 2× Laemmli buffer. Phosphorylated substrates are separated by 18% SDS-PAGE. The gels are dried and exposed to X-ray film for 3-10 min.
Cell Assay: 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 1×105 cells/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 exclusion.
Animal Administration: Bel-7402 tumor models: twenty female athymic (NCR-nu/nu) nude mice are injected with 1 × 107 Bel-7402 tumor cells subcutaneously, and 10-14 days later, when the tumor volumes reach 200-250 mm, the mice are divided into four groups such that each group harbors tumors of the same volume. Rigosertib (ON01910, 250 mg/kg) dissolved in PBS is administered alone or in combination with oxaliplatin (100 mg/kg) intraperitonially on alternate days. Tumor measurements are done two times/week using traceable digital vernier calipers. Body weight is determined during each measurement. The animals are observed for signs of toxicity[1].
References: [1]. Gumireddy K, et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell. 2005 Mar;7(3):275-86. [2]. Reddy MV, et al. Discovery of a clinical stage multi-kinase inhibitor sodium (E)-2-{2-methoxy-5-[(2',4',6'-trimethoxystyrylsulfonyl)methyl]phenylamino}acetate (ON 01910.Na): synthesis, structure-activity relationship, and biological activity. J Med Chem. [3]. Chapman CM, et al. ON 01910.Na is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Clin Cancer Res. 2012 Apr 1;18(7):1979-91
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