Rigosertib（Cat No.:I004219）is a small-molecule inhibitor targeting multiple pathways, primarily by inhibiting the Ras signaling pathway and disrupting the interaction of Ras with effector proteins. It primarily targets the serine/threonine kinase and phosphoinositide 3-kinase pathways, making it effective against various cancers, including myelodysplastic syndromes and solid tumors. Rigosertib induces cell cycle arrest and apoptosis in cancer cells, particularly those with Ras mutations or dysregulation. It has been evaluated in clinical trials, demonstrating potential as a treatment option for patients with hematological malignancies and other Ras-driven cancers.
| Catalog Number | I004219 |
| CAS Number | 592542-59-1 |
| Synonyms | 2-[2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]anilino]acetic acid |
| Molecular Formula | C21H25NO8S |
| Purity | ≥95% |
| Target | PLK |
| Solubility | DMSO 95 mg/mL; Water 95 mg/mL; Ethanol <1 mg/mL |
| Storage | Store at -20℃ |
| IC50 | 9 nM |
| IUPAC Name | 2-[2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]anilino]acetic acid |
| InChI | InChI=1S/C21H25NO8S/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)/b8-7+ |
| InChIKey | OWBFCJROIKNMGD-BQYQJAHWSA-N |
| SMILES | COC1=C(C=C(C=C1)CS(=O)(=O)/C=C/C2=C(C=C(C=C2OC)OC)OC)NCC(=O)O |
| Reference | <p style=/line-height:25px/> <br>[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. <br>[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. <br>[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. <br>[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. <br>[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. </p> |
