(E/Z)-Rigosertib sodium

SKU: orb1301101

Description

ON-01910 (Rigosertib) is a potent and selective non-ATP-competitive inhibitor of PLK1, demonstrating pro-apoptotic activity in cancer cells through PI3K/Akt pathway inhibition and oxidative stress induction. It is widely used in oncology research, with studies in both cellular and animal models exploring its mechanisms and therapeutic potential against various malignancies.

Research Area

Cell Biology

Key Properties

• CAS Number: 1225497-78-8
• MW: 473.47
• Purity: 99.82% (May vary between batches)
• Formula: C₂₁H₂₄NNaO₈S
• SMILES: [Na+].COc1cc(OC)c(C=CS(=O)(=O)Cc2ccc(OC)c(NCC([O-])=O)c2)c(OC)c1
• Target: PLK
• Solubility: DMSO:94 mg/mL (198.53 mM)

Bioactivity

• Target IC50:
  BCR-ABL:32 nM(Cell-free assay) |PLK1:9 nM(Cell-free assay) |Src:55 nM(Cell-free assay) |FLK1:42 nM(Cell-free assay) |PDGFR:18 nM(Cell-free assay)
• In Vivo:
  In vivo, this compound did not exhibit hematotoxicity, liver damage, or neurotoxicity, and was a potent inhibitor of tumor growth in a variety of xenograft nude mouse models. ON01910 showed strong synergy with several chemotherapeutic agents, often inducing complete regression of tumors.
• In Vitro:
  ON01910, a small molecule inhibitor of Plk1 activity, which induces mitotic arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis. This compound was not ATP-competitive, but competed for the substrate binding site of the enzyme.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

(E/Z) ON-01910 sodium, ON-01910, ON 01910, ON01910, PLK1

Compound Identifiers

PubChem CID

73265218