Home Categories Biochemical Engineering BAY87-2243
A1041250

BAY87-2243 , ≥98%(HPLC) , 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
5mg RMB552.00 In Stock
10mg RMB895.20 In Stock
25mg RMB1999.20 In Stock
50mg RMB3599.20 In Stock
100mg RMB6399.20 In Stock
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Update time: 2022-07-08

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.

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