BAY 87-2243

Catalog No.S7309

For research use only.

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.

BAY 87-2243 Chemical Structure

CAS No. 1227158-85-1

Selleck's BAY 87-2243 has been cited by 37 publications

Purity & Quality Control

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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 26500770
Growth inhibition assay Cell viability 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 (from reference)

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 525.53
Formula

C26H26F3N7O2

CAS No. 1227158-85-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=NN1CC2=CC(=NC=C2)N3CCN(CC3)C4CC4)C5=NC(=NO5)C6=CC=C(C=C6)OC(F)(F)F

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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.

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