Description
| 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) , FLK1:42 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)
