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(E/Z)-Rigosertib sodium

Catalog No. T6070   CAS 1225497-78-8
Synonyms: (E/Z) ON-01910 sodium

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
(E/Z)-Rigosertib sodium Chemical Structure
(E/Z)-Rigosertib sodium, CAS 1225497-78-8
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 55.00
10 mg In stock $ 97.00
25 mg In stock $ 193.00
50 mg In stock $ 363.00
100 mg In stock $ 622.00
1 mL * 10 mM (in DMSO) In stock $ 72.00
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Purity: 99.82%
Purity: 99.61%
Purity: 97.16%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 PDGFR:18 nM(Cell-free assay) , Flt1:42 nM(Cell-free assay) , PLK1:9 nM(Cell-free assay) , Bcr-Abl:32 nM(Cell-free assay) , Src:55 nM(Cell-free assay)
In vitro ON01910, a small molecule inhibitor of Plk1 activity, which induces mitotic arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis.?This compound was not ATP-competitive, but competed for the substrate binding site of the enzyme[1].
In vivo In vivo, this compound did not exhibit hematotoxicity, liver damage, or neurotoxicity, and was a potent inhibitor of tumor growth in a variety of xenograft nude mouse models.?ON01910 showed strong synergy with several chemotherapeutic agents, often inducing complete regression of tumors[1].
Synonyms (E/Z) ON-01910 sodium
Molecular Weight 473.47
Formula C21H24NNaO8S
CAS No. 1225497-78-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 94 mg/mL (198.53 mM)

TargetMolReferences 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:
Anti-Cancer Active Compound Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Anti-Viral Compound Library Anti-Cancer Compound Library Inhibitor Library Bioactive Compound Library Kinase Inhibitor Library

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Keywords

(E/Z)-Rigosertib sodium 1225497-78-8 Cell Cycle/Checkpoint PLK ON01910 ON-01910 ON 01910 (E/Z) ON-01910 sodium inhibitor inhibit

 

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