Rigosertib sodium

Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC 50 of 9 nM In Vitro Rigosertib is non-ATP-competitive inhibitor of PLK1 with IC 50 of 9 nM. Rigosertib also exhibits inhibition of PLK2, PDGFR, Flt1, BCR-ABL, Fyn, Src, and CDK1, with IC 50 of 18-260 nM. Rigosertib shows cell killing activity against 94 different tumor cell lines with IC 50 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 IC 50 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Rigosertib (200 mg/kg, i.p.) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Assay Tumor cells are plated into six-well dishes at a density of 1×10 5 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:PLK1 9 nM (IC 50 ) PLK2 260 nM (IC 50 ) PDGFR 18 nM (IC 50 ) Src 155 nM (IC 50 ) BCR-ABL 32 nM (IC 50 ) Cdk1 260 nM (IC 50 ) Flt1 42 nM (IC 50 ) Fyn 182 nM (IC 50 )

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