ONC212

Catalog No.S8673 Batch:S867301

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
* <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.)

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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, T_1/2 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

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

References

[4] Wagner J, et al. Cell Cycle. 2017, 16(19):1790-1799.

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Selleck's ONC212 has been cited by 4 publications

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
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.

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