Home Angiogenesis HIF inhibitor - ROS activator - Ferroptosis activator - Mitochondrial Metabolism inhibitor BAY 87-2243 For research use only.

BAY 87-2243

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

BAY 87-2243 Chemical Structure

CAS No. 1227158-85-1

Purity & Quality Control

BAY 87-2243 Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

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
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]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot NRF2 26500770
Growth inhibition assay Cell viability 26500770
In Vivo
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]
Animal Research Animal Models Mice bearing lung carcinoma H460 xenografts
Dosages ~4 mg/kg/d
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01297530 Terminated
Neoplasms
Bayer
 April 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 525.53 Formula

C26H26F3N7O2
CAS No. 1227158-85-1 SDF Download BAY 87-2243 SDF
Smiles CC1=CC(=NN1CC2=CC(=NC=C2)N3CCN(CC3)C4CC4)C5=NC(=NO5)C6=CC=C(C=C6)OC(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 50 mg/mL

DMSO : 16 mg/mL ( (30.44 mM) Warmed with 50°C water bath; Ultrasonicated; Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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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.

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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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