ONC212 |
Catalog No.GC34095
One-Click Copy Product Info
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ONC212, a chemical analogue of ONC201, is a fluorinated imipridone.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1807861-48-8
Sample solution is provided at 25 µL, 10mM.
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ONC212, a chemical analogue of ONC201, is a fluorinated imipridone[1]. ONC212 is a selective agonist of the orphan GPCR (G protein-coupled receptor) GPR132/G2A, with an EC50 of approximately 400nM[2]. ONC212 is commonly used in the study of pancreatic cancer[1], colorectal cancer[3], and acute myeloid leukemi[4].
ONC212 (5-20μM, 20-60μM; 48h) significantly reduced the number of viable cells in HeLa (IC50 = 16µM) and A549 (IC50 = 54µM) cells in a dose-dependent manner. ONC212 (5µM, 50µM; 48h) markedly increased early and late apoptosis in HeLa and A549 cells compared to their respective untreated controls[5].
ONC212 (50mg/kg/day; 23 days, 29 days; i.g.) exhibited significantly greater tumor growth inhibition than ONC201 in Capan-2 and PANC-1 xenograft models. ONC212 (50mg/kg, 3 times every week; 25 days, 54 days; i.g.) exhibited significantly greater tumor growth inhibition than the control group in the HPAF-II and BxPC-3 xenograft models[6].
References:
[1] Tajiknia V, Pinho-Schwermann M, Srinivasan P R, et al. Synergistic anti-tumor activity, reduced pERK, and immuno-stimulatory cytokine profiles with 5-FU or ONC212 plus KRAS G12D inhibitor MRTX1133 in CRC and pancreatic cancer cells independent of G12D mutation[J]. American Journal of Cancer Research, 2024, 14(9): 4523.
[2] Prabhu V V, Madhukar N, Tarapore R, et al. Potent anti-cancer effects of selective GPR132/G2A agonist imipridone ONC212 in leukemia and lymphoma[J]. Cancer Research, 2017, 77(13_Supplement): 1155-1155.
[3] Ferrarini I, Louie A, Zhou L, et al. ONC212 is a novel mitocan acting synergistically with glycolysis inhibition in pancreatic cancer[J]. Molecular cancer therapeutics, 2021, 20(9): 1572-1583.
[4] Nii T, Prabhu V V, Ruvolo V, et al. Imipridone ONC212 activates orphan G protein-coupled receptor GPR132 and integrated stress response in acute myeloid leukemia[J]. Leukemia, 2019, 33(12): 2805-2816.
[5] Basu V, Shabnam, Murghai Y, et al. ONC212, alone or in synergistic conjunction with Navitoclax (ABT-263), promotes cancer cell apoptosis via unconventional mitochondrial-independent caspase-3 activation[J]. Cell Communication and Signaling, 2024, 22(1): 441.
[6] Lev A, Lulla A R, Wagner J, et al. Anti-pancreatic cancer activity of ONC212 involves the unfolded protein response (UPR) and is reduced by IGF1-R and GRP78/BIP[J]. Oncotarget, 2017, 8(47): 81776.
| Cell experiment [1]: | |
Cell lines | Human cervical cell line HeLa and lung alveolar cancer cell line A549 |
Preparation Method | HeLa and A549 cells were seeded in 96 well plates. Subsequently, they were treated with ONC212 at different concentration ranges (5-20μM for HeLa cells and 20-60μM for A549 cells) for 48h. After treatment, MTT solution was added and incubated for 3h at 37°C. The solvent was added to dissolve the formazan crystal and after 30min, absorbance was measured at 590nm. |
Reaction Conditions | 5-20μM, 20-60μM; 48h |
Applications | ONC212 significantly reduced the number of viable cells in HeLa (IC50 = 16µM) and A549 (IC50 = 54µM) cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Human pancreatic cancer cell lines mouse model |
Preparation Method | Six- to seven-week-old female athymic nu/nu mice were acclimated for 1 week on arrival to the animal facility before in-vivo study was initiated. A total of 3-5×106 luciferase-expressing cells were suspended in 50μl of PBS mixed with 50μl of Matrigel and subcutaneously injected into the rear flanks of the mice. When tumor volume reached an average of 100-150cm3, mice were randomly assigned to the indicated control or treatment groups. ONC201 and ONC212 were delivered in a solution of 10% DMSO, 20% Kolliphor® EL, and 70% PBS by oral gavage at a dose of 50mg/kg, administered either daily (for PANC-1 and Capan-2 models) or three times a week (for HPAF-II and BxPC3 models). The length (L) and width (W) of the tumors were measured 1-2 times a week using a digital caliper, and the volume of the tumor was calculated using the formula: 0.5*L*W^2. Mice were also weighed once a week to monitor signs of drug toxicity. |
Dosage form | 50mg/kg, 3 or 7 times every week; 23 days, 25 days, 29 days, 54 days; i.g. |
Applications | ONC212 exhibited significantly greater tumor growth inhibition than ONC201 in Capan-2 and PANC-1 xenograft models. ONC212 exhibited significantly greater tumor growth inhibition than the control group in the HPAF-II and BxPC-3 xenograft models. |
References: | |
| Cas No. | 1807861-48-8 | SDF | |
| Canonical SMILES | O=C1N(CC2=CC=C(C(F)(F)F)C=C2)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4 | ||
| Formula | C24H23F3N4O | M.Wt | 440.46 |
| Solubility | DMSO : 50 mg/mL (113.52 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2704 mL | 11.3518 mL | 22.7035 mL |
| 5 mM | 454.1 μL | 2.2704 mL | 4.5407 mL |
| 10 mM | 227 μL | 1.1352 mL | 2.2704 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)