Molecular Formula | C26H26F3N7O2 |
Molar Mass | 525.53 |
Density | 1.47±0.1 g/cm3(Predicted) |
Boling Point | 677.7±65.0 °C(Predicted) |
Solubility | 10 mM in DMSO |
Appearance | solid |
Color | White |
pKa | 8.43±0.27(Predicted) |
Storage Condition | RT |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months. |
In vitro study | BAY87-2243 HIF-1 inhibition of reporter gene activity and CA9 protein expression, IC50 0.7 nM and 2 nM, respectively. In hypoxic lung cancer H460 cells, BAY 87-2243 inhibits HIF target gene expression and inhibits HIF-1α protein accumulation. Under glucose depletion, BAY 87-2243 inhibits cell proliferation by interfering with mitochondrial function. BAY87-2243 inhibited reporter gene activity and CA9 protein expression by HIF-1 with IC50 of 0.7 nM and 2 nM, respectively. In hypoxic lung cancer H460 cells, BAY 87-2243 inhibits HIF target gene expression and inhibits HIF-1α protein accumulation. Under glucose depletion, BAY 87-2243 inhibits cell proliferation by interfering with mitochondrial function. |
In vivo study | In the H460 xenograft mouse model, BAY87-2243(4 mg/kg P. O.) reduced tumor weight, HIF-1α protein, and HIF-1 target gene expression levels. In the H460 xenograft mouse model, BAY87-2243(4 mg/kg P. O.) reduced tumor weight, HIF-1α protein, and HIF-1 target gene expression levels. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.903 ml | 9.514 ml | 19.029 ml |
5 mM | 0.381 ml | 1.903 ml | 3.806 ml |
10 mM | 0.19 ml | 0.951 ml | 1.903 ml |
5 mM | 0.038 ml | 0.19 ml | 0.381 ml |