BAY 87-2243
- Product Name
- BAY 87-2243
- CAS No.
- 1227158-85-1
- Chemical Name
- BAY 87-2243
- Synonyms
- CS-1786;BAY 87-2243;BAY 87-2243 USP/EP/BP;BAY 87-2243 BAY87-2243;BAY87 2243;BAY 87 2243;BAY87-2243;Ferroptosis,inhibit,HIFs,HIF-PH,HIF/HIF Prolyl-Hydroxylase,Inhibitor,BAY 87-2243,BAY 872243,Hypoxia-inducible factors,BAY 87 2243;5-(1-((2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl)methyl)-5-methyl-1H-pyrazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole;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;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;Piperazine, 1-cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]-
- CBNumber
- CB22681993
- Molecular Formula
- C26H26F3N7O2
- Formula Weight
- 525.53
- MOL File
- 1227158-85-1.mol
BAY 87-2243 Property
- 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.
N-Bromosuccinimide Price
- Product number
- SML2384
- Product name
- BAY 87-2243
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $94.2
- Updated
- 2024/03/01
- Product number
- SML2384
- Product name
- BAY 87-2243
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $381
- Updated
- 2024/03/01
- Product number
- 28626
- Product name
- BAY 87-2243
- Packaging
- 5mg
- Price
- $81
- Updated
- 2024/03/01
- Product number
- 28626
- Product name
- BAY 87-2243
- Packaging
- 50mg
- Price
- $593
- Updated
- 2024/03/01
- Product number
- 28626
- Product name
- BAY 87-2243
- Packaging
- 10mg
- Price
- $152
- Updated
- 2024/03/01
BAY 87-2243 Chemical Properties,Usage,Production
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
Uses
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
BAY 87-2243 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from BAY 87-2243 manufacturers
- Product
- BAY 87-2243 1227158-85-1
- Price
- US $17.00/g
- Min. Order
- 1g
- Purity
- 95%
- Supply Ability
- 1KG
- Release date
- 2020-10-28