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Rigosertib sodium
- ON01910 sodium - Estybon- Parent CAS: 592542-59-1
- Soluble in water and DMSO
- MF: C21H24NNaO8S
- MW: 473.47
Description
Rigosertib sodium is a non-ATP-competitive inhibitor of PLK1 (IC50 value of 9–10 nM) which induces mitotic arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis. In vitro studies with Rigosertib sodium showed that incubation of human leukemic cells with this compound results in the inhibition of PI3K/AKT pathway, down regulation of cyclin D1, induction of NOXA and BIM and activation of JNK pathway. In vivo, Rigosertib sodium did not exhibit hematotoxicity, liver damage, or neurotoxicity, and was a potent inhibitor of tumor growth in a variety of xenograft nude mouse models.
More Information
| Parent CAS No. | 592542-59-1 |
|---|---|
| Chemical Name | Sodium (E)-2-(2-methoxy-5-((2,4,6-trimethoxystyrylsulfonyl)methyl)phenylamino)acetate |
| SMILES | C1C=C(CS(=O)(=O)/C=C/C2C(OC)=CC(OC)=CC=2OC)C=C(NCC(=O)[O-])C=1OC.[Na+] |
| MFCD | MFCD11655911 |
| InChi | InChI=1S/C21H25NO8S.Na/c1-27-15-10-19(29-3)16(20(11-15)30-4)7-8-31(25,26)13-14-5-6-18(28-2)17(9-14)22-12-21(23)24;/h5-11,22H,12-13H2,1-4H3,(H,23,24);/q;+1/p-1/b8-7+; |
| InChiKey | VLQLUZFVFXYXQE-USRGLUTNSA-M |
| CID | 23696523 |
| Short Description | PLK1 inhibitor |
References
- K Gumireddy et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell. 2005 Mar;7(3):275-86.
- MV Reddy et al. Discovery of a clinical stage multi-kinase inhibitor sodium (E)-2-{2-methoxy-5-[(2',4',6'-trimethoxystyrylsulfonyl)methyl]phenylamino}acetate (ON 01910.Na): synthesis, structure-activity relationship, and biological activity. J Med Chem. 2011 Sep 22;54(18):6254-76.
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