ONC212
Based on 5 publication(s) in Google Scholar
ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.86%
- No. CAS: 1807861-48-8
- Fòrmula: C24H23F3N4O
- Peso molecular:440.46
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) ONC212
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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IF
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Flow Cytometry
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WB
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Cell Imaging/Staining
Actividad biológica
GPR132[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.11 μM
Compound: ONC212
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 39172943] |
| HL-60 | IC50 |
0.09 μM
Compound: ONC212
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Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 39172943] |
| MIA PaCa-2 | IC50 |
0.1 μM
Compound: ONC212
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Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 39172943] |
| OCI-AML2 | IC50 |
76 nM
Compound: 35; ONC212
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Cytotoxicity against human OCI-AML2 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry
Cytotoxicity against human OCI-AML2 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry
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[PMID: 33656892] |
| OCI-AML-3 | IC50 |
60 nM
Compound: 35; ONC212
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Cytotoxicity against human OCI-AML-3 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry
Cytotoxicity against human OCI-AML-3 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry
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[PMID: 33656892] |
| SUM-159-PT | IC50 |
77 nM
Compound: 35; ONC212
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Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
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[PMID: 33656892] |
| Z-138 | IC50 |
49 nM
Compound: 35; ONC212
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Antiproliferative activity against human Z138 cells transfected with D190A mutant in NSG mouse assessed as tumor reduction at 50 mg/kg/d, po administered via oral gavage for every 2 day measured after 31 days by luminescence assay
Antiproliferative activity against human Z138 cells transfected with D190A mutant in NSG mouse assessed as tumor reduction at 50 mg/kg/d, po administered via oral gavage for every 2 day measured after 31 days by luminescence assay
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[PMID: 33656892] |
Cell proliferation assay reveals that at least a ten-fold lower concentration of ONC212 is needed to achieve 50% growth inhibition in comparison to ONC201. ONC212 shows GI50 values in the range of 0.1 to 0.4 μM, while the corresponding ONC201 GI50 values are in the range of 4 to 9 μM for the seven pancreatic cancer cell lines tested. Long-term cell proliferation assay shows that both ONC201 and ONC212 are comparable in inhibiting colony formation at a 20 μM dose. However, at a 5 μM dose, ONC212 is about 50-times more potent than ONC201 in preventing colony formation in four out of the seven pancreatic cancer cell lines tested. Induction of apoptosis by ONC212 is an earlier event than ONC201. Treatment with ONC201 and ONC212 reduces the expression of anti-apoptotic markers such as XIAP and MCL-1. Western blot analysis shows that in the HPAF-II cell line, ATF4 and phosphorylated EIF2α are upregulated as early as 6 to 12 hours post ONC201 or ONC212 treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ONC212 treatment exhibits significantly greater growth inhibition in comparison to ONC201. A dose of 50 mg/kg of ONC212 administered three-times a week is sufficient to lead to significant growth inhibition of tumors compare to the control group for these two models. Results demonstrate that ONC212 treated tumors show reduced proliferation in the HPAF-II model[2].
In vivo toxicity assessment experiments show that ONC212 is well tolerated up to 250 mg/kg. 300 mg/kg of ONC212 causes splenic damage and elevates liver enzymes. ONC212 has a slightly shorter half-life than ONC201, with a clearance from the blood at 12 hours, T1/2 of 4.3 hours, and Cmax of 1.4 μg/mL[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1807861-48-8
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Appearance Solid
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Peso molecular 440.46
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Fòrmula C24H23F3N4O
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Color White to off-white
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SMILES
O=C1N(CC2=CC=C(C(F)(F)F)C=C2)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Autophagy
2026 Mar 5. PMID: 41787744 -
Cell Commun Signal
ONC212, alone or in synergistic conjunction with Navitoclax (ABT-263), promotes cancer cell apoptosis via unconventional mitochondrial-independent caspase-3 activation. [Abstract]2024 Sep 13;22(1):441. PMID: 39272099
ONC212 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Sep 13;22(1):441. [Abstract]
The viability of HeLa was determined by MTT assay at different concentrations (5 to 20 μM) of ONC212 treatment for 48 h. The IC50 value was calculated to be 16.3 μM.
ONC212 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Sep 13;22(1):441. [Abstract]
Hoechst-stained pictures of ONC212 (15 μM for Hela，and 50 μM for A549)-induced nuclear condensation.
ONC212 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Sep 13;22(1):441. [Abstract]
Representative flow cytometry scatter plots of Annexin-V FITC/PI staining in control and ONC212-treated cells. ONC212 (15 μM for Hela，and 50 μM for A549) treatment increased the proportion of early and late apoptotic cell populations compared to untreated control.
ONC212 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Sep 13;22(1):441. [Abstract]
The western blot demonstrated that ONC212 (15 μM for Hela，and 50 μM for A549) treatment gradually (24 h and 48 h) induced effective caspase-3 and PARP cleavage in both HeLa and A549 cancer cells. Caspase-8 cleavage did not occur upon ONC212 treatment.
ONC212 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Sep 13;22(1):441. [Abstract]
Clonogenicity assay showing the survival efficacy of cancer cells after ONC212 (15 μM for Hela，and 50 μM for A549) treatment for 48 h.
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Biochem Pharmacol
ONC212 enhances YM155 cytotoxicity by triggering SLC35F2 expression and NOXA-dependent MCL1 degradation in acute myeloid leukemia cells. [Abstract]2024 Jun:224:116242. PMID: 38679209 -
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Solvente y solubilidad
DMSO : 50 mg/mL (113.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 20% Cremophor EL 70% ddH2O
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
All pancreatic cancer cell lines are treated with ONC201 or ONC212 at the indicated doses and time-points. Post-treatment, both floating and adherent cells are collected, fixed in 70% ethanol and stained with propidium iodide in the presence of ribonuclease A. Flow cytometric data is collected using a flow cytometer. The sub-G1 fraction (apoptotic) is quantified, and analysis is performed to quantify the distribution of cells in G1, S and G2-M phases of the cell cycle utilizing[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Six- to seven-week-old female athymic nu/nu mice are used in this study. A total of 3 to 5×106 luciferase-expressing cells are suspended in 50 μL of PBS mixed with 50 μL of Matrigel and subcutaneously injected into the rear flanks of the mice. When tumor volume reaches an average of 100 to 150 cm3, mice are randomly assigned to the indicated control or treatment groups. ONC201 and ONC212 are delivered in a solution of 10% DMSO, 20% Kolliphor®EL and 70% PBS by oral gavage. The length (L) and width (W) of the tumors are measured 1 to 2 times a week using a digital caliper, and the volume of the tumor is calculated. Mice are also weighed once a week to monitor signs of drug toxicity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (701 KB)
- English - EN (701 KB)
- Français - FR (701 KB)
- Deutsch - DE (701 KB)
- Norwegian - NO (701 KB)
- Español - ES (701 KB)
- Swedish - SV (701 KB)
- Italian - IT (701 KB)
- Korean - KR (701 KB)
- Portuguese - PT (701 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[2]. Lev A, et al. Anti-pancreatic cancer activity of ONC212 involves the unfolded protein response (UPR) and is reduced by IGF1-R and GRP78/BIP. Oncotarget. 2017 Sep 12;8(47):81776-81793. [Content Brief]
[3]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2704 mL | 11.3518 mL | 22.7035 mL | 56.7588 mL |
| 5 mM | 0.4541 mL | 2.2704 mL | 4.5407 mL | 11.3518 mL | |
| 10 mM | 0.2270 mL | 1.1352 mL | 2.2704 mL | 5.6759 mL | |
| 15 mM | 0.1514 mL | 0.7568 mL | 1.5136 mL | 3.7839 mL | |
| 20 mM | 0.1135 mL | 0.5676 mL | 1.1352 mL | 2.8379 mL | |
| 25 mM | 0.0908 mL | 0.4541 mL | 0.9081 mL | 2.2704 mL | |
| 30 mM | 0.0757 mL | 0.3784 mL | 0.7568 mL | 1.8920 mL | |
| 40 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4190 mL | |
| 50 mM | 0.0454 mL | 0.2270 mL | 0.4541 mL | 1.1352 mL | |
| 60 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9460 mL | |
| 80 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7095 mL | |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5676 mL |
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