Molecular Weight(MW): 525.53
BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.
Cited by 14 Publications
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Fresh human PMP tissue was exposed to HIF-1α inhibitor (BAY 87-2243) under hypoxic conditions in vitro for 24 hours. MUC2 mRNA levels as measured by real-time PCR (F) and MUC2 protein expression as measured by immunofluorescence staining (G) were significantly reduced by the inhibitor; for immunofluorescence assay slides were stained with MUC2 antibody (green IF) and SYTOX Orange for nucleic acid (blue IF). Confocal images were randomly taken of 10 different fields (X 63 magnification) and analyzed using Image-pro Premier Software to quantify the average intensity of MUC2 expression.
Transl Res, 2016, doi:10.1016/j.trsl.2015.10.006. BAY 87-2243 purchased from Selleck.
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.
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|Description||BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.|
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. 
|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. |
|In vitro||DMSO||33 mg/mL warmed (62.79 mM)|
|Ethanol||8 mg/mL warmed (15.22 mM)|
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Frequently Asked Questions
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?
Solutol is a non-ionic solubilizer and emulsifier used in making vehicle formulations.