ONC212

Catalog No.S8673 Batch:S867301

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Technical Data

Formula

C24H23F3N4O
Molecular Weight 440.46 CAS No. 1807861-48-8
Solubility (25°C)* In vitro DMSO 88 mg/mL (199.79 mM)
Ethanol 88 mg/mL (199.79 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.2mg/ml Taking the 1 mL working solution as an example, add 50 μL of 44 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
1.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 28 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.
In vitro ONC212 shows an anti-proliferative effect in a large panel of pancreatic cancer cell lines with ONC212 having at least a ten-fold increased potency than ONC201. ONC212 induces apoptosis earlier and at lower concentrations than ONC201 in sensitive pancreatic cancer cell lines[1]. ONC212 exerts potent and prominent apoptogenic effects on acute myeloid leukemia (AML) and mantle cell lymphoma (MCL) cell lines (e.g., ED50s of 141.0 nM in p53 wild-type OCI-AML3 cells, 105.7 nM in MOLM13 cells, and 265.2 nM in p53-null JeKo-1 cell lines). Time course analysis of apoptosis in OCI-AML3 cells shows that ONC212 takes more than 36 hours to start to induce apoptosis[2]. ONC212 significantly induces Sub-G1 apoptotic cells and/or cell cycle arrest[4].
In vivo ONC212 shows improved efficacy in melanoma and hepatocellular carcinoma xenograft models[1]. ONC212 has a broad therapeutic window, an acceptable PK profile, and is orally well-tolerated in mice with no evidence of toxicity at efficacious doses in both colon and triple negative breast cancer[3]. ONC212 exhibits rapid kinetics of activity. 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 mg/mL. It has a prolonged pharmacodynamic effect despite systemic clearance. Oral ONC212 shows potent anti-tumor efficacy in a human melanoma xenograft and hepatocellular model. ONC206 and ONC201 both inhibit invasion and migration of tumor cells while ONC212 inhibits only invasion[4].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    PANC-1 and HPAF-Ⅱ cells

  • Concentrations

    5 µM or 20 µM

  • Incubation Time

    72 h

  • Method

    Colony formation assays are performed by seeding 0.2 × 106 cells/well in a 6-well plate and treatment with indicated doses of ONC201 or ONC212. At 72 hours post-treatment, cells are harvested and 500 cells per treatment group are plated in drug-free media in triplicate for colony formation. Colonies are stained with 0.25% crystal violet on Day 10, imaged, counted and reported as number of colonies ± SEM.
Animal Study:

[1]
  • Animal Models

    PANC-1, Capan-2, HPAF-II and BxPC3 xenograft models (athymic nu/nu mice)

  • Dosages

    50 mg/kg

  • Administration

    by oral gavage

Selleck's ONC212 has been cited by 7 publications

BMP2 and BMP7 cooperate with H3.3K27M to promote quiescence and invasiveness in pediatric diffuse midline gliomas [ Elife, 2024, 12RP91313] PubMed: 39373720
Untersuchung zur Wirkung von tumortherapeutisch relevanten Imipridonderivaten auf den spannungsabhängigen Natriumkanal hNav1. 5 [ OPARU, 2023, 10.18725/OPARU-48122] PubMed: none
Characterization of TR-107, a novel chemical activator of the human mitochondrial protease ClpP [ Pharmacol Res Perspect, 2022, 10(4):e00993] PubMed: 35929764
Small molecule clpp agonists induce senescence and alter trail-mediated apoptotic response of triple-negative breast cancer cells [ BioRxiv, 2022, 10.1101/2022.07.11.499620] PubMed: None
Targeting Mitochondrial Metabolism in Clear Cell Carcinoma of the Ovaries [ Int J Mol Sci, 2021, 22(9)4750] PubMed: 33947138
Block of Voltage-Gated Sodium Channels as a Potential Novel Anti-cancer Mechanism of TIC10 [ Front Pharmacol, 2021, 12:737637] PubMed: 34744721
Targeting Mitochondria in Melanoma [ Biomolecules, 2020, 10(10)E1395] PubMed: 33007949

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.