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Purity: =99.95%
ONC206 (ONC-206; ONC 206), an analogue of ONC201 (TRAIL inducer) and benzyl-flurobenzyl imipridone, is a novel, potent and selective antagonist of the D2-like dopamine receptors (DRD2/3/4) with a broad-spectrum of anticancer activity.
| ln Vitro |
In contrast to D1 samples (DRD 1/5), ONC206 is selective against D2 samples (DRD2/3/4) [2]. Tumor cell migration and toxins are strongly inhibited by ONC206 [1]. 0.05 μM; over 48 hours) does not cause cell death or limit cell proliferation, but rather inhibits the migration of ONC201 and TRAIL-activated HCT116 Bax migration cells [1]. ISR and TRAIL trapping, which induces tumor development and cell death, is mediated by ONC206 [1]. Induced cells in the cell proliferation experiment for colorectal cell lines do not develop ONC201 resistance in ONC206 [1].
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| ln Vivo |
Onc206 (100 mg/kg; sidewall every ten times) significantly inhibits the growth of tumors [2].
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: HCT116 Cell Tested Concentrations: 0.05 μM Incubation Duration: over 48 hrs (hours) Experimental Results: Inhibition of ONC201- and TRAIL-resistant HCT116 Bax−/− Cell migration. |
| References |
[1]. Wagner J, et al. Preclinical evaluation of the imipridone family, analogs of clinical stage anti-cancer small molecule ONC201, reveals potent anti-cancer effects of ONC212. Cell Cycle. 2017 Oct 2;16(19):1790-1799.
[2]. Varun Vijay Prabhu, et al. Potent anti-cancer activity of the imipridone ONC206: A selective dopamine D2-like receptor antagonist. AACR Annual Meeting 2017, April 1-5, 2017; Washington, DC. |
| Molecular Formula |
C23H22F2N4O
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|---|---|
| Molecular Weight |
408.4528
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| Exact Mass |
408.176
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| CAS # |
1638178-87-6
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| SMILES |
FC1C([H])=C(C([H])=C([H])C=1C([H])([H])N1C(C2C([H])([H])N(C([H])([H])C3C([H])=C([H])C([H])=C([H])C=3[H])C([H])([H])C([H])([H])C=2N2C([H])([H])C([H])([H])N=C21)=O)F
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| Synonyms |
ONC 206 ONC-206 ONC206
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~244.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (7.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3.25 mg/mL (7.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3.25 mg/mL (7.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (24.48 mM) in Cremophor EL (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4483 mL | 12.2414 mL | 24.4828 mL | |
| 5 mM | 0.4897 mL | 2.4483 mL | 4.8966 mL | |
| 10 mM | 0.2448 mL | 1.2241 mL | 2.4483 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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