BAY 87-2243

Price	$17
Package	1g

Product Details

Product Name: BAY 87-2243	CAS No.: 1227158-85-1
Min. Order: 1g	Purity: 95%
Supply Ability: 1KG	Release date: 2021/01/06
Name: Cassie Guo

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

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)

Safety Information

MSDS Information

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 ).

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