Product Details
- Product NameBAY 87-2243
- CAS No.1227158-85-1
- MFC26H26F3N7O2
- MW525.53
- AppearancesolidWhite
- Boiling point 677.7±65.0 °C(Predicted)
- density 1.47±0.1 g/cm3(Predicted)
- storage temp. RT
| BAY 87-2243 Basic information |
| Product Name: |
BAY 87-2243 |
| Synonyms: |
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 BAY87-2243;BAY 87-2243;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;CS-1786;BAY87 2243;BAY 87 2243;BAY87-2243 |
| CAS: |
1227158-85-1 |
| MF: |
C26H26F3N7O2 |
| MW: |
525.5255496 |
| EINECS: |
|
| Product Categories: |
Inhibitors |
| Mol File: |
1227158-85-1.mol |
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| BAY 87-2243 Chemical Properties |
| Boiling point |
677.7±65.0 °C(Predicted) |
| density |
1.47±0.1 g/cm3(Predicted) |
| pka |
8.43±0.27(Predicted) |
| |
| BAY 87-2243 Usage And Synthesis |
| 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. |
Company Profile
Introduction
Technology research and transfer of pilot screening, pilot scale-up and mass production solutions , for pharmaceutical intermediates, biologicals and fine chemicals (Not including inflammable , explosive , hazardous goods ) ; Market : Nano material , metal catalyst , raw material of cosmetics , pharmaceutical intermediates , chemicals , photoelectric material , import and export of technology and goods (For projects subject to approval according to law, business activities can be carried out only after approval by relevant departments ).
