Contact us: +91 9550333722 040 - 40102781
Structured search
India
Choose your country
Different countries will display different contents
Try our best to find the right business for you.
My chemicalbook

Welcome back!

HomeProduct name listBAY 87-2243

BAY 87-2243

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

BAY 87-2243 Structural

What is BAY 87-2243?

Description

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

The Uses of BAY 87-2243

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.

Enzyme inhibitor

This Hif1a inhibitor (FW = 525.53 g/mol; CAS 1227158-85-1; Solubility: <1 mg/mL DMSO or H2O) targets the transcription factor hypoxia-inducible factor-1 (HIF-1), which plays an essential role in tumor development, tumor progression, and resistance to chemo- and radiotherapy. BAY 87-2243 inhibits HIF-1α and HIF-2α accumulation under hypoxic conditions in the H460 Non-Small Cell Lung Cancer (NSCLC) cell line but is without effect on HIF-1α protein levels that are induced by such hypoxia mimetics asdesferrioxamine or cobalt chloride. BAY 87-2243 has no effect on HIF target gene expression levels in RCC4 cells lacking Von Hippel-Lindau (VHL) activity; nor does it affect the activity of HIF prolyl hydroxylase-2. Antitumor activity of BAY 87-2243, suppression of HIF-1α protein levels, and reduction of HIF-1 target gene expression in vivo have been demonstrated in a H460 xenograft model. BAY 87-2243 does not inhibit cell proliferation under standard conditions. Upon glucose depletion, a condition favoring mitochondrial ATP generation as energy source, BAY 87-2243 inhibits cell proliferation in the low-nM range. In a mouse model for BRAF mutant melanoma, BAY 87-2243-mediated complex I inhibition induces melanoma cell death in vitro and reduces melanoma tumor growth in various mouse models in vivo. This effect is mediated through BAY 87-2243- induced stimulation of mitochondrial ROS production, leading to oxidative damage and subsequent cell death. BAY 87-2243 displays increased anti tumor efficacy compared to single agent treatment, when combined with the BRAF inhibitor vemurafenib in nude mice with BRAF mutant melanoma xenografts.

storage

Store at -20°C

References

1) Ellinghaus?et al.?(2013),?BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I; Cancer Med.,2?611 2) Schockel?et al.?(2015),?Targeting mitochondrial complex I using BAY 87-2243 reduces melanoma tumor growth; Cancer Metab.,?3?11 3) Basit?et al.?(2017),?Mitochondrial complex I inhibition triggers a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis in melanoma cells; Cell Death Discov.,?8?e2716

Properties of BAY 87-2243

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).
form  solid
pka 8.43±0.27(Predicted)
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.

Safety information for BAY 87-2243

Computed Descriptors for BAY 87-2243

Related products of tetrahydrofuran

You may like

  • BAY 87-2243 CAS 1227158-85-1
    BAY 87-2243 CAS 1227158-85-1
    1227158-85-1
    View Details
  • 1-Methyl-6-oxo-1,6-dihydropyridazine-3-carbonitrile 98%
    1-Methyl-6-oxo-1,6-dihydropyridazine-3-carbonitrile 98%
    99903-60-3
    View Details
  • 1823368-42-8 98%
    1823368-42-8 98%
    1823368-42-8
    View Details
  • 2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    1307449-08-6
    View Details
  • Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    25408-95-1
    View Details
  • 2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    1805639-70-6
    View Details
  • 1784294-80-9 98%
    1784294-80-9 98%
    1784294-80-9
    View Details
  • Lithium Clavulanate
    Lithium Clavulanate
    61177-44-4
    View Details
Statement: All products displayed on this website are only used for non medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.