- Home
- Signaling Pathways
- Cell Cycle/Checkpoint
- PLK
- Rigosertib sodium salt
Rigosertib sodium salt
Rigosertib (ON-01910,Estybon) is a potent, specific PLK1 inhibitor with IC50 value of 9nM. Rigosertib strongly inhibited the proliferation of cancer cell lines, with observed IC50 values in the nanomolar range for both HeLa (115 nM) and C33A (45 nM) cells. In contrast, rigosertib had a minimal effect on normal cell lines, BJ and Ect1/E6E7 (IC50 > 0.1 mM) [1]
HeLa and C33A cells demonstrated a complete (>95%) G2/M arrest at concentrations of rigosertib >0.5 μM, whereas at
Rigosertib has been reported to be a more potent radiosensitizer than cisplatin in vivo [1].
Reference:
[1]?Agoni?L1,?Basu?I2,?Gupta?S3,?Alfieri?A2,?Gambino?A4,?Goldberg?GL5,?Reddy?EP6,?Guha?C7.Rigosertib?is?a?more?effective?radiosensitizer?than?cisplatin?in?concurrent?
chemoradiation?treatment?of?cervical?carcinoma,?in?vitro?and?in?vivo.?Int?J?Radiat?Oncol?Biol?Phys.?2014?Apr?1;88(5):1180-7.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 473.47 |
| Cas No. | 1225497-78-8 |
| Formula | C21H24NNaO8S |
| Synonyms | ON-01910,Estybon |
| Solubility | ≥23.65 mg/mL in DMSO; insoluble in EtOH; ≥52.3 mg/mL in H2O |
| Chemical Name | sodium;2-[2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]anilino]acetate |
| SDF | Download SDF |
| Canonical SMILES | COC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)[O-].[Na+] |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Kinase experiment [1]: | |
|
In vitro enzyme assays for PLK1 |
Recombinant PLK1 (10 ng) was 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 mins at room temperature. Kinase reactions were performed for 20 mins at 30 °C in a volume of 20 μL of reaction mixture (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 were terminated by boiling for 2 mins in 20 μL of 2× Laemmli buffer. Phosphorylated substrates were separated by 18% SDS-PAGE. The gels were dried and exposed to X-ray film for 3 ~ 10 mins. |
| Cell experiment [1]: | |
|
Cell lines |
HeLa cells |
|
Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
250 nM; 8, 12, 16, 20 or 28 hrs |
|
Applications |
In HeLa cells, Rigosertib significantly inhibited PLK1 activity at all stages of the cell cycle. Moreover, the loss of PLK1 activity was not due to degradation of PLK1 or inhibition of PLK1 synthesis. |
| Animal experiment [1]: | |
|
Animal models |
Nude mice bearing Bel-7402, MCF-7 or MIA-PaCa cell xenografts |
|
Dosage form |
250 mg/kg; i.p. |
|
Applications |
In nude mice bearing Bel-7402, MCF-7 or MIA-PaCa cell xenografts, Rigosertib (250 mg/kg) significantly inhibited tumor growth without obvious toxicity. In addition, Rigosertib completely inhibited PLK1 activity but partially reduced CDK1 activity. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Gumireddy K, Reddy MV, Cosenza SC, Boominathan R, Baker SJ, Papathi N, Jiang J, Holland J, Reddy EP. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell. 2005 Mar;7(3):275-86. |
|
| Description | Rigosertib is a non-ATP-competitive small-molecule inhibitor of Plk1 with IC50 value of 9 nM. | |||||
| Targets | Plk1 | |||||
| IC50 | 9 nM | |||||
Quality Control & MSDS
- View current batch:
Chemical structure
