BAY 87-2243

$ 17.00 /1g

Min. Order1g
Purity95%
Cas No1227158-85-1
Supply Ability1KG
Update time2024-10-22

Career Henan Chemica Co

5YR

China

Chemical Properties

Product Name	BAY 87-2243
CAS No	1227158-85-1
EC-No
Min. Order	1g
Purity	95%
Supply Ability	1KG
Release date	2024/10/22

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.

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