Rigosertib

• CAT Number: I004219
• CAS Number: 592542-59-1
• Molecular Formula: C21H25NO8S
• Molecular Weight: 451.49
• Purity: ≥95%
• Target: PLK
• Solubility: DMSO 95 mg/mL; Water 95 mg/mL; Ethanol <1 mg/mL
• Storage: Store at -20℃
• IC50: 9 nM [1]
• 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=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)O

Rigosertib (Cat.No:I004219) is an investigational anticancer drug that belongs to the class of small-molecule inhibitors targeting Ras signaling pathways. It selectively inhibits the enzyme Ras-related C3 botulinum toxin substrate (RAC1), which plays a critical role in cancer cell proliferation and survival. Rigosertib has shown promise in preclinical studies and clinical trials for various cancers, making it a potential candidate for targeted cancer therapy.

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.