BAY 87-2243

製品コードS7309 バッチS730903

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	C₂₆H₂₆F₃N₇O₂
	分子量	525.53	CAS No.	1227158-85-1
Solubility (25°C)*	体外	Ethanol	5 mg/mL warmed with 50ºC water bath (9.51 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	BAY 87-2243 は、強力かつ選択的な低酸素誘導因子-1 (HIF-1) 阻害剤です。BAY 87-2243 はミトコンドリア複合体 I 活性を阻害し、それによってマイトファジー依存性の ROS 増加を引き起こし、ネクロプトーシスとフェロトーシスを誘発します。BAY 87-2243 は抗腫瘍活性を発揮します。第1相。
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, this compound suppresses HIF target gene expression, and inhibits HIF-1α protein accumulation. Under glucose depletion, it inhibits cell proliferation via interference with mitochondrial function.
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.

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. This compound 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.

参考

https://pubmed.ncbi.nlm.nih.gov/24403227/

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：

Hypoxia Inhibitor Improves Iodine Uptake Disorder in Thyroid Cancer Through the hsa_circ_0023990/miR-448/DNMT1/NIS Axis [ Cancer Sci, 2025, 116(8):2113-2124]	PubMed: 40386902
Hypoxia Inhibitor Improves Iodine Uptake Disorder in Thyroid Cancer Through the hsa_circ_0023990/miR-448/DNMT1/NIS Axis [ Cancer Sci, 2025, 10.1111/cas.70102]	PubMed: 40386902
Attenuation of palmitic acid-induced lysyl oxidase overexpression in the ovary contributes to the improvement of ovulation in obesity by metformin [ Hum Reprod Open, 2024, 2024(1):hoae002]	PubMed: 38333108
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

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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