ONC213
Based on 1 Customer Validation
ONC213 is an orally active αKGDH inhibitor. ONC213 can suppress mitochondrial respiration and elevate α-ketoglutarate levels by inhibiting αKGDH activity. ONC213 can induce cells apoptosis by inducing mitochondrial stress response and inhibiting translation of MCL-1. ONC213 can be used for the research of cancer, such as acute myeloid leukemia research (AML).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.86%
- CAS 番号: 1977540-13-8
- 分子式: C23H22F2N4O
- 分子量:408.44
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[1]|
Caspase 3 |
体外実験
ONC213 (500 nM, 48 h) reduces colony formation in primary AML samples[1].
ONC213 (125-1000 nM, 48 h) induces apoptosisi in MV4-11, OCI-AML3, and MOLM-13 cells[1].
ONC213 (250-500 nM, 8 h) strongly suppresses maximal OCR and spare respiratory capacity, with a minimal effect on basal respiration in MV4-11 and THP-1 cells[1].
ONC213 (500 nM, 0.5-16 h) inhibits activity of α-KGDH in MV4-11 cells[1].
ONC213 (250-500 nM, 4-8 h) induces mitochondrial stress gene expression in MV4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MV4-11, OCI-AML3, and MOLM-13 cells
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Concentration:125, 250, 500 and 1000 nM
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Incubation Time:48 h
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Result:Increased apoptotic/dead cells.
Increased cleavage of caspase 3 and PARP.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11 xenografted mice models[1]
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Dosage:75 and 125 mg/kg
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Administration:Orally administration, daily for 8 days
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Result:Increased median survival to 43.5 days from 33 days at75 mg/kg.
Nearly doubled survival from 33 to 62 days at125 mg/kg.
化学情報
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CAS 番号 1977540-13-8
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性状 Solid
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分子量 408.44
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分子式 C23H22F2N4O
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Color Off-white to light yellow
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SMILES
O=C1N(CC2=CC=C(F)C(F)=C2)C3=NCCN3C4=C1CN(CC4)CC5=CC=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (244.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
純度とドキュメンテーション
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データシート (272 KB)
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取扱説明書 (2659 KB)
参考文献
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4483 mL | 12.2417 mL | 24.4834 mL | 61.2085 mL |
| 5 mM | 0.4897 mL | 2.4483 mL | 4.8967 mL | 12.2417 mL | |
| 10 mM | 0.2448 mL | 1.2242 mL | 2.4483 mL | 6.1209 mL | |
| 15 mM | 0.1632 mL | 0.8161 mL | 1.6322 mL | 4.0806 mL | |
| 20 mM | 0.1224 mL | 0.6121 mL | 1.2242 mL | 3.0604 mL | |
| 25 mM | 0.0979 mL | 0.4897 mL | 0.9793 mL | 2.4483 mL | |
| 30 mM | 0.0816 mL | 0.4081 mL | 0.8161 mL | 2.0403 mL | |
| 40 mM | 0.0612 mL | 0.3060 mL | 0.6121 mL | 1.5302 mL | |
| 50 mM | 0.0490 mL | 0.2448 mL | 0.4897 mL | 1.2242 mL | |
| 60 mM | 0.0408 mL | 0.2040 mL | 0.4081 mL | 1.0201 mL | |
| 80 mM | 0.0306 mL | 0.1530 mL | 0.3060 mL | 0.7651 mL | |
| 100 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6121 mL |
ONC213 関連分類
HY-164515 関連分類
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