BAY 87-2243

Catalog No.S7309 Batch:S730903

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Technical Data

Formula

C26H26F3N7O2
Molecular Weight 525.53 CAS No. 1227158-85-1
Solubility (25°C)* In vitro Ethanol 5 mg/mL (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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
HIF-1 [1]
(Cell-free assay)
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]

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    Non-small cell lung cancer (NSCLC) cell line H460

  • Concentrations

    10 μM

  • Incubation Time

    48 hours

  • Method

    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.
Animal Study:[1]
  • Animal Models

    Mice bearing lung carcinoma H460 xenografts

  • Dosages

    ~4 mg/kg/d

  • Administration

    p.o.

Customer Product Validation

, , 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's BAY 87-2243 has been cited by 47 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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