BAY 87-2243

For research use only.

Catalog No.S7309

32 publications

BAY 87-2243 Chemical Structure

CAS No. 1227158-85-1

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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Selleck's BAY 87-2243 has been cited by 32 publications

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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]

Assay
Methods Test Index PMID
Western blot
NRF2; 

PubMed: 26500770     


Melanoma cells were treated with BAY 87-2243 (10 nM). Cell lysates were collected from treated melanoma cell lines (8 h) and probed with antibodies recognizing NRF2. Actin was used as a loading control.

26500770
Growth inhibition assay
Cell viability; 

PubMed: 26500770     


BRAF wild type and mutant melanoma cells were treated with various concentrations of BAY 87-2243. Cell viability was measured after 72 h. IC50 values were calculated using GraphPad prism (n = 4).

26500770
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

Cell Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Mice bearing lung carcinoma H460 xenografts
  • Dosages: ~4 mg/kg/d
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 33 mg/mL warmed (62.79 mM)
Water Insoluble
Ethanol '8 mg/mL warmed

* 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.

Chemical Information

Molecular Weight 525.53
Formula

C26H26F3N7O2

CAS No. 1227158-85-1
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC(=NN1CC2=CC(=NC=C2)N3CCN(CC3)C4CC4)C5=NC(=NO5)C6=CC=C(C=C6)OC(F)(F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01297530 Terminated Drug: BAY87-2243 Neoplasms Bayer April 2011 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    How to formulate the compound for mouse in vivo experiment? I noticed that "For in vivo studies, BAY 87-2243 was formulated in a 1% (v/v) solution of ethanol/solutol/water (10/40/50%). Animals were given BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) or vehicle control once daily by oral gavage" referred from Cancer Medicine 2013; 2(5): 611–624. What is solutol?

  • Answer:

    Solutol is a non-ionic solubilizer and emulsifier used in making vehicle formulations.

HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID