BAY 87-2243, Hypoxia-inducible Factor-1 (HIF-1) Inhibitor


Catalog No. size PriceQuantity
M60217-2S 2 mg solid $119
M60217-10S 10mg solid $482

Description

Product Information
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.
Purity: ≥98%
CAS#: 1227158-85-1
Molecular Weight: 525.53
Formula: C26H26F3N7O22
Solubility: DMSO up to 1 mM; EtOH up to 15 mM (heating)
Chemical Name: 5-(1-((2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl)methyl)-5-methyl-1H-pyrazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole

 

Biological Activity:

BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. It inhibits HIF-1 reporter gene activity and target gene CA9 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. BAY 87-2243 had no effect on HIF target gene expression levels in RCC4 cells lacking Von Hippel-Lindau (VHL) activity nor did the compound affect the activity of HIF prolyl hydroxylase-2. Antitumor activity of BAY 87-2243, suppression of HIF-1α protein levels, and reduction of HIF-1 target gene expression in vivo were demonstrated in a H460 xenograft model. BAY 87-2243 is currently in phase I clinical trials. 

 

How to Use:

In vitro:  BAY 87-2243 was used at 0.1-10 µM final concentration in various in vitro assays.

In vivo: BAY 87-2243 was dosed to Mice bearing lung carcinoma H460 xenografts via oral gavage at 4 mg/kg once per day. Formulation is 1% (v/v) solution of ethanol/solutol/water (10/40/50%). 

 

Reference:

 

  1.  Ellinghaus P, et al. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. (2013) Cancer Med. 2(5):611-24.
Products are for research use only. Not for human use. 

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