1. Metabolic Enzyme/Protease
    Apoptosis
  2. HIF/HIF Prolyl-Hydroxylase
    Ferroptosis
  3. BAY 87-2243

BAY 87-2243 

Cat. No.: HY-15836 Purity: 99.69%
Handling Instructions

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

For research use only. We do not sell to patients.

BAY 87-2243 Chemical Structure

BAY 87-2243 Chemical Structure

CAS No. : 1227158-85-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 132 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 114 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 624 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1152 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BAY 87-2243 purchased from MCE. Usage Cited in: Radiother Oncol. 2015 Sep;116(3):431-7.

    Radiation-induced Hif1α expression and blockage by BAY87-2243 or EGFR siRNA. A549 and FaDu cells are pretreated with BAY87-2243 or hypoxia and irradiated with 2 Gy. Six hours after irradiation, cells are lysed, and Western blotting is performed.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    HIF-1α[1]

    In Vitro

    BAY 87-2243 inhibits luciferase activity with a calculated IC50 value of ~0.7 nM. Hypoxic induction of the HIF target gene CA9 on protein level in HCT116luc cells is inhibited by BAY 87-2243 with an IC50 value of ~2 nM. BAY 87-2243 inhibits mitochondrial oxygen consumption measured by using the oxygen sensitive fluorescence dye LUX-MitoXpress with an IC50 value of ~10 nM[1]. BAY-87-2243 inhibits nuclear HIF-1α protein expression. Administration of BAY-87-2243 for about 18 days significantly reduces HIF-1α protein expression as well as pimonidazole hypoxic fraction (pHF) (mean 2.4% (BAY-87-2243) vs. 17.6% (carrier), p<0.0001), and necrotic fraction (NF) (mean 9% vs. 35.6%, p=0.0002), whereas relative vascular area (RVA) and perfused vessels (PF) remained unchanged[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Nude mice are inoculated with H460 cells subcutaneously and after tumors have been established, animals are treated with BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) for 3 weeks by daily oral gavage. BAY 87-2243 reduced tumor weight dose dependently in line with a dose-dependent reduction of the mRNA expression levels of the HIF-1 target genes CA9, ANGPTL4, and EGLN3, whereas the mRNA expression levels of hypoxia-insensitive EGLN2 gene and of HIF-1α itself are not affected by compound treatment in vivo[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    525.53

    Formula

    C₂₆H₂₆F₃N₇O₂

    CAS No.
    SMILES

    FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC(N5CCN(C6CC6)CC5)=NC=C4)C(C)=C3)=N2)C=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (47.57 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9028 mL 9.5142 mL 19.0284 mL
    5 mM 0.3806 mL 1.9028 mL 3.8057 mL
    10 mM 0.1903 mL 0.9514 mL 1.9028 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    Luciferase activity is given in % of DMSO-treated cells. 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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice[1]
    Tumor xenograft experiment is carried out on female immune-deficient, athymic NMRI nude mice, aged 7-9 weeks, weighing 20-25 g. The lung carcinoma xenograft mouse model is established by subcutaneous injection into the right flank with 0.1 mL H460 tumor cells (1.5×106) mixed 1:1 with Matrigel. Mice are randomized into control and BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) groups when tumors reach a size of more than 40 mm2. Body weight is monitored as a measure for treatment-related, acute toxicity. Tumor area (measured by caliper) or tumor weight (measured when mice are sacrificed 21 days after cell injection) is calculated by the formula 100-100×(tumor weight/area of treatment group)/(tumor weight/area of vehicle group). Tumor Statistical analysis is performed using the one-way analysis of variance.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.69%

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    Keywords:

    BAY 87-2243HIF/HIF Prolyl-HydroxylaseFerroptosisHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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    Product Name:
    BAY 87-2243
    Cat. No.:
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