1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase

BAY 87-2243 

Cat. No.: HY-15836 Purity: 99.41%
Data Sheet SDS 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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $110 In-stock
5 mg $95 In-stock
10 mg $120 In-stock
50 mg $520 In-stock
100 mg $960 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    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.

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    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].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Cell Assay
    [1]

    BAY 87-2243 is dissolved in DMSO (10 mM) and stored, and then diluted with the relevant assay media before use[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]

    BAY 87-2243 is formulated in a 1% (v/v) solution of ethanol/solutol/water (10/40/50%) (Mice)[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
    Molecular Weight

    525.53

    Formula

    C₂₆H₂₆F₃N₇O₂

    CAS No.

    1227158-85-1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.41%

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    Inquiry Information

    Product Name:
    BAY 87-2243
    Cat. No.:
    HY-15836
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