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Rigosertib

Chemical Structure : Rigosertib

CAS No.: 592542-59-1

Rigosertib (ON-01910;ON01910;ON 01910)

Catalog No.: PC-42852Not For Human Use, Lab Use Only.

Rigosertib (ON 01910) is a potent, non-ATP-competitive PLK1 inhibitor (IC50=9-10 nM), selectively induces mitotic G2/M arrest and apoptosis in cancer cells.

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Biological Activity

Rigosertib (ON 01910) is a potent, non-ATP-competitive PLK1 inhibitor (IC50=9-10 nM), selectively induces mitotic G2/M arrest and apoptosis in cancer cells.
Rigosertib (ON 01910) also exhibits inhibitory activity against PDGFR, Abl, and Flt-1, at higher concentrations, inhibits CDK1, Plk2, Src, and Fyn.
Rigosertib (ON 01910) demonstrates in vitro cytotoxicity against DU145 and K562 cells with IC50 of 100 and 15 nM.
Rigosertib (ON 01910) potently inhibits tumor growth in a variety of xenograft nude mouse models, does not exhibit hematotoxicity, liver damage, or neurotoxicity shows strong synergy with several chemotherapeutic agents.

Physicochemical Properties

M.Wt 451.4901
Formula C21H25NO8S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Glycine, N-[2-methoxy-5-[[[(1E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]-

References

1. Reddy MV, et al. J Med Chem. 2011 Sep 22;54(18):6254-76.

2. Gumireddy K, et al. Cancer Cell. 2005 Mar;7(3):275-86.

3. Oussenko IA, et al. Cancer Res. 2011 Jul 15;71(14):4968-76.

4. Chun AW, et al. Cancer Chemother Pharmacol. 2009 Dec;65(1):177-86.

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