product name BAY 87-2243
Description: BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. It 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.
References: Cancer Med. 2013 Oct;2(5):611-24.
525.53
Formula
C26H26F3N7O2
CAS No.
1227158-85-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: <1 mg/mL
Ethanol: 8 mg/mL (15.22 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1942656
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: Cells were plated at 3 × 10E4 cells/well and incubated overnight before BAY 87-2243 (5 mmol/L in DMSO) were added and plates were placed in a hypoxic chamber for 16 h at 1% pO2. Results are given as luminescence counts in arbitrary units after subtraction of baseline levels from normoxic, nontreated controls. For the measurement of cellular complex I activity, H1299 cells were cotransfected with a pcDNA3 vector encoding for Pyrearinus termitilluminans larval click beetle luciferase. Clones (H1299tluc) showing high luminescence and dose-dependent rotenone sensitivity were subcloned and then used for further in depth analysis of cellular complex I activity by luminescence measurements. |
|---|---|
| In Vivo | Nude mice were inoculated with H460 cells subcutaneously and after tumors have been established, animals were treated with BAY 87-2243 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 were not affected by compound treatment in vivo. H460 cells was inhibited by BAY 87-2243 with an EC50 of ~3 nmol/L, indicating that BAY 87-2243 is an inhibitor of mitochondrial function. |
| Animal model | Mice bearing lung carcinoma H460 xenografts |
| Formulation & Dosage | Formulated in 1% (v/v) solution of ethanol/solutol/water (10/40/50%); 4 mg/kg/d; p.o. |
| References | Cancer Med. 2013 Oct;2(5):611-24. |
