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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $34 | In Stock | |
5 mg | $55 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $193 | In Stock | |
50 mg | $363 | In Stock | |
100 mg | $622 | In Stock | |
1 mL x 10 mM (in DMSO) | $72 | In Stock |
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) , Src:55 nM(Cell-free assay) , BCR-ABL:32 nM(Cell-free assay) , PLK1:9 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]. |
Alias | (E/Z) ON-01910 sodium |
Molecular Weight | 473.47 |
Formula | C21H24NNaO8S |
Cas No. | 1225497-78-8 |
Smiles | [Na+].COc1cc(OC)c(C=CS(=O)(=O)Cc2ccc(OC)c(NCC([O-])=O)c2)c(OC)c1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 94 mg/mL (198.53 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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