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Cell Cycle/Checkpoint PLK ON-01910

ON-01910

Catalog No. T6070   CAS 1225497-78-8
Synonyms: Rigosertib, Estybon

ON-01910 is a non-ATP-competitive PLK1 inhibitor(IC50 of 9 nM, in a cell-free assay). It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells.It is a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity.

ON-01910, CAS 1225497-78-8
Pack Size Availability Price/USD Quantity
2 mg In stock 97.00
5 mg In stock 140.00
10 mg In stock 269.00
25 mg In stock 482.00
50 mg In stock 818.00
1 mL * 10 mM (in DMSO) In stock 151.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description ON-01910 is a non-ATP-competitive PLK1 inhibitor(IC50 of 9 nM, in a cell-free assay). It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells.It is a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity.
Targets&IC50 PLK1 : ic50 9nM,  
Kinase Assay 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.
Cell Research
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
Animal Research
Animal Model: Mouse (feathymic, NCR-nu/nu) xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells
Synonyms Rigosertib , Estybon
Purity 99.82%
Molecular Weight 473.47
Formula C21H24NNaO8S
CAS No. 1225497-78-8

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 94 mg/mL (198.53 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

Saline: 30 mg/mL

Citations

References and Literature
1. Gumireddy K , Reddy M V R , Cosenza S C , et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent.[J]. Cancer Cell, 2005, 7(3):275-286. 2. Dai, Yi-Han, Lai, et al. ON 01910.Na inhibits growth of diffuse large B-cell lymphoma by cytoplasmic sequestration of sumoylated C-MYB/TRAF6 complex[J]. Translational Research the Journal of Laboratory & Clinical Medicine, 2016.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Cell cycle related Compound Library

Related Products

Related compounds with same targets
ON-01910 Rigosertib TC-S 7005 Poloxime Poloxin 7-O-Prenylscopoletin ON-01910 HMN176

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