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BAY 87-2243 HIF inhibitor

Cat.No.S7309

BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. This compound inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. It exerts antitumor activity. Phase 1.

Chemical Structure

Molecular Weight: 525.53

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Quality Control

Batch: Purity: 99.67%

99.67

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src FLT FLT3 HER2 Bcr-Abl
Other HIF Inhibitors	PT2399 PX-478 Dihydrochloride KC7F2 Lificiguat (YC-1) IOX2 CAY10585 (LW 6) Molidustat (BAY 85-3934) PT2385 IDF-11774 MK-8617

Solubility

In vitro
Batch:

Ethanol : 50 mg/mL

DMSO : 16 mg/mL (30.44 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.950mg/ml (1.81mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.950mg/ml (1.81mM)

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	525.53	Formula	C₂₆H₂₆F₃N₇O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1227158-85-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Mechanism of Action

Targets/IC₅₀/Ki	HIF-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, 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24403227/

Applications

Methods	Biomarkers	Images	PMID
Western blot	NRF2		26500770
Growth inhibition assay	Cell viability		26500770

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01297530	Terminated	Neoplasms	Bayer	April 2011	Phase 1

Tech Support

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, it was formulated in a 1% (v/v) solution of ethanol/solutol/water (10/40/50%). Animals were given this compound (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:
It is a non-ionic solubilizer and emulsifier used in making vehicle formulations.

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