BAY 87-2243

製品コードS7309 バッチS730902

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26H26F3N7O2
分子量 525.53 CAS No. 1227158-85-1
Solubility (25°C)* 体外 Ethanol 50 mg/mL warmed with 50ºC water bath (95.14 mM)
DMSO Insoluble
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.

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生物活性

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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Non-small cell lung cancer (NSCLC) cell line H460
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.

カスタマーフィードバック

, , 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.]

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：

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。

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