ONC206

SKU: orb1307929

Description

ONC206 is a nanomolar-potency antagonist of D2-like dopamine receptors (DRD2/3/4) and a structural analog of the TRAIL-inducing compound ONC201. It exhibits broad-spectrum anti-tumor activity, supporting its investigation in both in vitro and in vivo cancer research models for oncology and neuro-oncology applications.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1638178-87-6
• MW: 408.44
• Purity: 99.93% (May vary between batches)
• Formula: C₂₃H₂₂F₂N₄O
• SMILES: Fc1ccc(CN2C3=NCCN3C3=C(CN(Cc4ccccc4)CC3)C2=O)c(F)c1
• Target: Dopamine Receptor
• Solubility: DMSO:103 mg/mL (252.18 mM)

Bioactivity

• In Vivo:
  ONC206 (100 mg/kg; p.o.; every 10 days) reduces obviously tumor growth inhibition.
• In Vitro:
  ONC206 (Oncoceutics) is an imipiridone with nanomolar potency and analogue of ONC201, a selective dopamine receptor D2 (DRD2) antagonist currently being investigated in phase II clinical trials for serous endometrial cancer (SEC). ONC206 inhibited cellular proliferation in a dose-dependent manner and was more potent than ONC201 in the ARK1 (IC50 = 0.33 M vs. IC50 = 1.59uM) and SPEC-2 (IC50 = 0.24uM vs. IC50 = 0.81uM) cell lines. Treatment with ONC206 resulted in induction of ROS production and reduction of mitochondrial membrane potential, accompanied by an increase in cleaved caspase-3 and caspase-9 activity (p < 0.01). ONC206 also significantly inhibited cellular adhesion and migration in both cell lines (p < 0.01). Pretreatment with the stress inhibitor N-acetylcysteine (NAC) significantly attenuated the efficacy of ONC206 on cell proliferation, ROS production and cellular invasion. ONC206 demonstrates nanomolar potency for the inhibition of proliferation in SEC cells.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, ONC 206, ONC201, ONC206, ONC-206, antagonist, D2-like, DRD2/3/4, DopamineReceptor, dopamine, Dopamine, Dopamine Receptor, receptors

Compound Identifiers

PubChem CID

135297777