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ONC206, an analogue of the TRAIL inducer ONC201, acts as a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations and possesses broad-spectrum anti-tumor activity.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $29 | In Stock | In Stock | |
| 5 mg | $46 | In Stock | In Stock | |
| 10 mg | $76 | In Stock | In Stock | |
| 25 mg | $123 | In Stock | In Stock | |
| 50 mg | $221 | In Stock | In Stock | |
| 100 mg | $329 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $43 | In Stock | In Stock |
| Description | ONC206, an analogue of the TRAIL inducer ONC201, acts as a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations and possesses broad-spectrum anti-tumor activity. |
| 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[3]. |
| In vivo | ONC206 (100 mg/kg; p.o.; every 10 days) reduces obviously tumor growth inhibition[2]. |
| Molecular Weight | 408.44 |
| Formula | C23H22F2N4O |
| Cas No. | 1638178-87-6 |
| Smiles | Fc1ccc(CN2C3=NCCN3C3=C(CN(Cc4ccccc4)CC3)C2=O)c(F)c1 |
| Relative Density. | 1.36 g/cm3 (Predicted) |
| 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. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 103 mg/mL (252.18 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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