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> ONC212 [1807861-48-8]

ONC212 [1807861-48-8]

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Cat# HY-111343-5mg

Size : 5mg

Brand : MedChemExpress

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Description

ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis[1].

IC50 & Target

GPR132[1]
Cellular Effect
Cell Line Type Value Description References
OCI-AML2 IC50
76 nM
Compound: 35; ONC212
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
[PMID: 33656892]
OCI-AML-3 IC50
60 nM
Compound: 35; ONC212
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
[PMID: 33656892]
SUM-159-PT IC50
77 nM
Compound: 35; ONC212
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
[PMID: 33656892]
Z-138 IC50
49 nM
Compound: 35; ONC212
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
[PMID: 33656892]
In Vitro

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 Related Antibodies

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2704 mL 11.3518 mL 22.7035 mL
5 mM 0.4541 mL 2.2704 mL 4.5407 mL
View the 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.

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    20% Cremophor EL    70% ddH2O

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

  • Protocol 2

    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.
Purity & Documentation
References

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