BAY87-2243 , 10mMinDMSO , 1227158-85-1
Synonym(s):
1-Cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]piperazine;1-Cyclopropyl-4-{4-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)methyl]pyridin-2-yl}piperazine
CAS NO.：1227158-85-1
Empirical Formula: C26H26F3N7O2
Molecular Weight: 525.53
MDL number: MFCD28143915
| Pack Size | Price | Stock | Quantity |
| 1ml | RMB559.20 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Boiling point: | 677.7±65.0 °C(Predicted) |
| Density | 1.47±0.1 g/cm3(Predicted) |
| storage temp. | RT |
| solubility | Soluble in DMSO (up to 25 mg/ml) or in Ethanol (10 mg/ml). |
| pka | 8.43±0.27(Predicted) |
| form | solid |
| color | White |
| 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. |
Description and Uses
BAY 87-2243 (1227158-85-1) potently inhibits HIF-1 reporter gene activity (IC50?= 0.7 nM) and CA9 protein expression (IC50?= 2.0 nM).1?It inhibited HIF-1α and HIF-2α protein accumulation in hypoxic H460 cells and reduced tumor weight in nude mice inoculated with H460 cells. BAY 87-2243 potently inhibits mitochondrial complex I activity (IC50?= 10 nM in mitochondria isolated from PC3 cells) leading to its HIF-1 effects. It has no effect on mitochondrial complex III. BAY 87-2243 reduced melanoma tumor growth?via?its targeting of mitochondrial complex I.2,3
BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced gene activation. It is found to inhibit HIF-1α and HIF-2α protein accumulation under hypoxic conditions in non-small cell lung cancer cell line H460. It inhibits mitochondrial complex I activity and therefore may be used in antitumor treatment to overcome chemo- and radiotherapy- resistance of hypoxic tumors.
