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BAY 87-2243

BAY 87-2243 Suppliers list
Company Name: ATK CHEMICAL COMPANY LIMITED
Tel: +86 21 5161 9050/ 5187 7795
Email: ivan@atkchemical.com
Products Intro: Product Name:BAY 87-2243
CAS:1227158-85-1
Purity:98% HPLC Package:5MG;10MG;50MG;100MG,1G,5G
Company Name: Biochempartner
Tel: 0086-13720134139
Email: candy@biochempartner.com
Products Intro: Product Name:BAY 87-2243
CAS:1227158-85-1
Purity:98% HPLC LCMS Package:10G;20G
Company Name: Hubei Jusheng Technology Co.,Ltd.
Tel: 86-18871470254
Email: linda@hubeijusheng.com
Products Intro: Product Name:BAY 87-2243
CAS:1227158-85-1
Purity:0.99 Package:5KG;1KG
Company Name: BOC Sciences
Tel: 1-631-619-7922
Email: inquiry@bocsci.com
Products Intro: Product Name:BAY 87-2243
CAS:1227158-85-1
Purity:>98%
Company Name: Amadis Chemical Company Limited
Tel: 0086-571-89925085
Email: sales@amadischem.com
Products Intro: Product Name:BAY 87-2243
CAS:1227158-85-1
Purity:0.97 Package:mgs,gs,kgs Remarks:A900651
BAY 87-2243 Basic information
Product Name:BAY 87-2243
Synonyms:BAY87 2243;BAY 87 2243;BAY87-2243;CS-1786;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
CAS:1227158-85-1
MF:C26H26F3N7O2
MW:525.5255496
EINECS:
Product Categories:Inhibitors
Mol File:1227158-85-1.mol
BAY 87-2243 Structure
BAY 87-2243 Chemical Properties
Boiling point 677.7±65.0 °C(Predicted)
density 1.47±0.1 g/cm3(Predicted)
pka8.43±0.27(Predicted)
Safety Information
MSDS Information
BAY 87-2243 Usage And Synthesis
Enzyme inhibitorThis 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.
BAY 87-2243 Preparation Products And Raw materials
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