Rigosertib

• Description :

  Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle[1][2]. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM[3].

• CAS Number :

  [592542-59-1]

• Product Name Alternative :

  ON-01910

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Apoptosis; PI3K; Polo-like Kinase (PLK)

• Type :

  Reference compound

• Related Pathways :

  Apoptosis; Cell Cycle/DNA Damage; PI3K/Akt/mTOR

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/rigosertib.html

• Purity :

  99.01

• Solubility :

  DMSO : 75 mg/mL (ultrasonic)

• Smiles :

  COC1=CC=C(C=C1NCC(O)=O)CS(/C=C/C2=C(C=C(C=C2OC)OC)OC)(=O)=O

• Molecular Formula :

  C21H25NO8S

• Molecular Weight :

  451.49

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Xu F, et al. Rigosertib as a selective anti-tumor agent can ameliorate multiple dysregulated signalingtransduction pathways in high-grade myelodysplastic syndrome. Sci Rep. 2014 Dec 4;4:7310.|[2]Hyoda T, et al. Rigosertib induces cell death of a myelodysplastic syndrome-derived cell line by DNA damage-induced G2/M arrest. Cancer Sci. 2015 Mar;106 (3) :287-93.|[3]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.|[4]Reddy MV, 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.|[5]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

• Shipping Conditions :

  Blue Ice

• Storage Conditions :

  -20°C (Powder, stored under nitrogen)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 3

• Isoform :

  PLK1; PLK2

• Citation 01 :

  Harvard Medical School LINCS LIBRARY|Int J Biol Sci. 2020 Jun 27;16 (13) :2382-2391.|Oncogenesis. 2025 Mar 1;14 (1) :4.|Oncol Res. 2021 Sep 7;28 (7) :745-761.|Sci Rep. 2017 Aug 17;7 (1) :8629. |Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Harvard Medical School LINCS LIBRARY