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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26H26F3N7O2 |
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分子量 | 525.53 | CAS No. | 1227158-85-1 | ||||||||
Solubility (25°C)* | 体外 | DMSO (warmed with 50ºC water bath) | 19 mg/mL (36.15 mM) | ||||||||
Ethanol (warmed with 50ºC water bath) | 8 mg/mL (15.22 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. BAY 87-2243 inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. BAY 87-2243 exerts antitumor activity. Phase 1. |
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in vitro | BAY 87-2243 inhibits HIF-1 reporter gene activity and CA9 protein expression with IC50 of 0.7 nM and 2 nM, respectively. In hypoxic lung cancer H460 cells, BAY 87-2243 suppresses HIF target gene expression, and inhibits HIF-1α protein accumulation. Under glucose depletion, BAY 87-2243 inhibits cell proliferation via interference with mitochondrial function. [1] |
in vivo | In H460 xenograft mouse model, BAY 87-2243 (4 mg/kg p.o.) reduces tumor weight, HIF-1α protein, and HIF-1 target gene expression levels. [1] |
細胞アッセイ | 細胞株 | Non-small cell lung cancer (NSCLC) cell line H460 |
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濃度 | 10 μM | |
反応時間 | 48 hours | |
実験の流れ | To evaluate the cytotoxicity of BAY 87-2243, 2.000 cells of the respective cell lines are seeded in 96-well plates and cultured in the appropriate growth medium containing 10% FCS. BAY 87-2243 at various concentrations is added at 24 h after seeding for additional 48 h and cell viability is determined using Cell Titer Glow Assay. | |
動物実験 | 動物モデル | Mice bearing lung carcinoma H460 xenografts |
投薬量 | ~4 mg/kg/d | |
投与方法 | p.o. |
, , Oncotarget, 2016, 7(52):86313-86325
Data from [Data independently produced by , , Transl Res, 2016, doi:10.1016/j.trsl.2015.10.006]
Data from [Data independently produced by , , Vascul Pharmacol, 2016, 83:47-56.]
Forchlorfenuron-Induced Mitochondrial Respiration Inhibition and Metabolic Shifts in Endometrial Cancer [ Cancers (Basel), 2024, 16(5)976] | PubMed: 38473335 |
HIF-1 inhibition reverses opacity in a rat model of galactose-induced cataract [ PLoS One, 2024, 19(2):e0299145] | PubMed: 38416732 |
Hypoxia-induced downregulation of microRNA-186-5p in endothelial cells promotes non-small cell lung cancer angiogenesis by upregulating protein kinase C alpha [ Mol Ther Nucleic Acids, 2023, 31:421-436] | PubMed: 36845338 |
Histone acetyltransferase P300 deficiency promotes ferroptosis of vascular smooth muscle cells by activating the HIF-1α/HMOX1 axis [ Mol Med, 2023, 29(1):91] | PubMed: 37415103 |
Gelatin methacryloyl (GelMA) loaded with concentrated hypoxic pretreated adipose-derived mesenchymal stem cells(ADSCs) conditioned medium promotes wound healing and vascular regeneration in aged skin [ Biomater Res, 2023, 27(1):11] | PubMed: 36782342 |
ACSL4 deficiency confers protection against ferroptosis-mediated acute kidney injury [ Redox Biol, 2022, 51:102262] | PubMed: 35180475 |
System analysis based on the cancer-immunity cycle identifies ZNF207 as a novel immunotherapy target for hepatocellular carcinoma [ J Immunother Cancer, 2022, 10(3)e004414] | PubMed: 35246476 |
Short isoform thymic stromal lymphopoietin reduces inflammation and aerobic glycolysis of asthmatic airway epithelium by antagonizing long isoform thymic stromal lymphopoietin [ Respir Res, 2022, 23(1):75] | PubMed: 35351157 |
Activation of transcription factor HIF inhibits IL-1β-induced NO production in primary cultured rat hepatocytes [ Nitric Oxide, 2022, 124:1-14] | PubMed: 35460897 |
Hypoxia-induced myeloid derived growth factor promotes hepatocellular carcinoma progression through remodeling tumor microenvironment [ Theranostics, 2021, 11(1):209-221] | PubMed: 33391471 |
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。