ONC212

製品コードS8673 バッチS867301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₄H₂₃F₃N₄O

分子量

440.46

CAS No.

1807861-48-8

Solubility (25°C)*

体外

DMSO

88 mg/mL (199.79 mM)

Ethanol

88 mg/mL (199.79 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.200mg/ml (4.99mM)	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 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.400mg/ml (3.18mM)	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	フッ素化ONC201アナログであるONC212は、GPR132の選択的アゴニストです。ONC212は、ほとんどの固形腫瘍および血液悪性腫瘍に対して低ナノモル範囲で広く有効であり、強力な抗白血病活性を有します。
in vitro	ONC212 shows an anti-proliferative effect in a large panel of pancreatic cancer cell lines with this compound having at least a ten-fold increased potency than ONC201. It induces apoptosis earlier and at lower concentrations than ONC201 in sensitive pancreatic cancer cell lines. This compound 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 it takes more than 36 hours to start to induce apoptosis. This chemical significantly induces Sub-G1 apoptotic cells and/or cell cycle arrest.
in vivo	ONC212 shows improved efficacy in melanoma and hepatocellular carcinoma xenograft models. This compound 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. It exhibits rapid kinetics of activity. This chemical 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 administration 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 this compound inhibits only invasion.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PANC-1 and HPAF-Ⅱ cells
	濃度	5 µM or 20 µM
	反応時間	72 h
	実験の流れ	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.
動物実験	動物モデル	PANC-1, Capan-2, HPAF-II and BxPC3 xenograft models (athymic nu/nu mice)
	投薬量	50 mg/kg
	投与方法	by oral gavage

参考

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5669847/
http://www.bloodjournal.org/content/128/22/4059
http://cancerres.aacrjournals.org/content/77/13_Supplement/3245

https://pubmed.ncbi.nlm.nih.gov/28489985/

+ 展开

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Raphin-1 mediates the survival and sensitivity to radiation of pediatric-type diffuse high-grade glioma via phosphorylated eukaryotic initiation factor 2α-dependent and -independent processes [ Mol Oncol, 2025, 10.1002/1878-0261.70081]	PubMed: 40632659
ONC201 enhances the cytotoxic effect of cisplatin through ATF3/ATF4/CHOP in head and neck squamous cell carcinoma cells [ Oncogenesis, 2025, 14(1):20]	PubMed: 40533448
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
Profiling the Multi-Omic Response to Mitochondrial Protease ClpP Activation in Triple-Negative Breast Cancer Cells [ proquest, 2022, ]	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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。