BAY 87-2243

Catalog No.S7309

BAY 87-2243 Chemical Structure

Molecular Weight(MW): 525.53

BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.

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1 Customer Review

  • Quiescent VSMC were pretreated with 10 or 30 μM HIF inhibitor BAY 87-2243 and then stimulated with PDGF (10 ng/mL) for 6 h. Total cell lysates were subjected to immunoblot analysis for HK2 and actin. Representative blots and compiled densitometric data from three independent experiments are depicted (n = 3, mean + SD.; * p b 0.05; ANOVA, Bonferroni).

    Vascul Pharmacol, 2016, 83:47-56.. BAY 87-2243 purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. 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

Cell Research
+ Expand
  • 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
+ Expand
  • Animal Models: Mice bearing lung carcinoma H460 xenografts
  • Formulation: 1% (v/v) solution of ethanol/solutol/water (10/40/50%)
  • Dosages: ~4 mg/kg/d
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 8 mg/mL (15.22 mM) warming
DMSO <1 mg/mL
Water <1 mg/mL
In vivo

* 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.

Chemical Information

Molecular Weight 525.53
Formula

C26H26F3N7O2

CAS No. 1227158-85-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01297530 Terminated 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