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

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.
• InChIKey: CDJNNOJINJAXPV-UHFFFAOYSA-N
• SMILES: N1(C2CC2)CCN(C2=NC=CC(CN3C(C)=CC(C4ON=C(C5=CC=C(OC(F)(F)F)C=C5)N=4)=N3)=C2)CC1

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.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H315-H319-H335
• Precautionary statements: P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501