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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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||Ethanol||8 mg/mL (15.22 mM) warming|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01297530||Terminated||Neoplasms||Bayer||April 2011||Phase 1|
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