Rigosertib sodium

• CAT Number: I004220
• CAS Number: 592542-60-4
• Molecular Formula: C21H24NNaO8S
• Molecular Weight: 473.47
• Purity: ≥95%
• Synonyms: sodium;2-[2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]anilino]acetate
• Target: PLK
• Solubility: H2O: ≥ 52 mg/mL
• Storage: Store at -20C
• IC50: 9 nM
• 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
• SMILES: COC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)[O-].[Na+]

Rigosertib sodium（Cat No.:I004220）is a multi-kinase inhibitor that primarily targets the Ras/Raf signaling pathway, disrupting multiple signaling cascades essential for cancer cell survival and proliferation. It inhibits polo-like kinase 1 (PLK1) and phosphoinositide 3-kinase (PI3K), leading to cell cycle arrest and apoptosis in cancer cells. Rigosertib sodium is being investigated for its potential in treating myelodysplastic syndromes (MDS) and other hematological malignancies. Its ability to selectively target cancer cells while sparing normal cells makes it a promising agent in cancer therapy, particularly for resistant or refractory cancers.

Reference

[1]. Gumireddy K, 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.
[2]. Chapman CM, et al. ON 01910.Na is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Clin Cancer Res. 2012 Apr 1;18(7):1979-91.
[3]. Oussenko IA, et al. Effect of ON 01910.Na, an anticancer mitotic inhibitor, on cell-cycle progression correlates with RanGAP1 hyperphosphorylation. Cancer Res. 2011 Jul 15;71(14):4968-76.
[4]. Chun AW, et al. Preclinical pharmacokinetics and in vitro activity of ON 01910.Na, a novel anti-cancer agent. Cancer Chemother Pharmacol. 2009 Dec;65(1):177-86.
[5]. Jimeno A, et al. Phase I study of ON 01910.Na, a novel modulator of the Polo-like kinase 1 pathway, in adult patients with solid tumors. J Clin Oncol. 2008 Dec 1;26(34):5504-10.
[6]. Komrokji RS, et al. Phase I clinical trial of oral rigosertib in patients with myelodysplastic syndromes. Br J Haematol. 2013 Aug;162(4):517-24.