Molecular Weight(MW): 473.47
Rigosertib (ON-01910) 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. Phase 3.
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|Description||Rigosertib (ON-01910) 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. Phase 3.|
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. |
In vitro enzyme assays for PLK1: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.
|In vitro||DMSO||95 mg/mL (200.64 mM)|
|Water||95 mg/mL (200.64 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02075034||Suspended||Drug: rigosertib||Myelodysplastic Syndrome||Onconova Therapeutics Inc.||May 2014||Phase 1|
|NCT02030639||Completed||Drug: rigosertib||Healthy||Onconova Therapeutics Inc.||January 2014||Phase 1|
|NCT01928537||Active not recruiting||Drug: rigosertib sodium||Myelodysplastic Syndromes|Refractory Anemia With Excess Blasts|Chronic Myelomonocytic Leukemia|Cytopenia||Onconova Therapeutics Inc.||August 2013||Phase 3|
|NCT01807546||Completed||Drug: rigosertib||Head and Neck Squamous Cell Carcinoma|Anal Squamous Cell Carcinoma|Lung Squamous Cell Carcinoma|Cervical Squamous Cell Carcinoma|Esophageal Squamous Cell Carcinoma|Skin Squamous Cell Carcinoma|Penile Squamous Cell Carcinoma||Onconova Therapeutics Inc.||March 2013||Phase 2|
|NCT01168011||Completed||Drug: rigosertib||Solid Tumor||Onconova Therapeutics Inc.||July 2010||Phase 1|
|NCT01167166||Completed||Drug: rigosertib||Acute Myelocytic Leukemia|Acute Lymphocytic Leukemia|Myeloproliferative Disease|Chronic Myeloid Leukemia||Onconova Therapeutics Inc.||July 2010||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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