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BAY 87-2243

化学構造式
1227158-85-1
CAS番号.
1227158-85-1
化学名:
别名:
英語名:
BAY 87-2243
英語别名:
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
化学式:
C26H26F3N7O2
分子量:
525.53
MOL File:
1227158-85-1.mol
MSDS File:
SDS

BAY 87-2243 物理性質

沸点 :
677.7±65.0 °C(Predicted)
比重(密度) :
1.47±0.1 g/cm3(Predicted)
貯蔵温度 :
RT
溶解性:
DMSO (最大 25mg/ml) またはエタノール (10mg/ml) に可溶。
酸解離定数(Pka):
8.43±0.27(Predicted)
外見 :
個体
色:
白い
安定性：:
-20°C の DMSO またはエタノール溶液で最大 2 か月間保存できます。

安全性情報

BAY 87-2243 価格 もっと(2)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
Sigma-Aldrich Japan SML2384 ≥98% (HPLC)
BAY 87-2243 ≥98% (HPLC)		 1227158-85-1 5MG ￥11300 2023-06-01 購入
Sigma-Aldrich Japan SML2384 ≥98% (HPLC)
BAY 87-2243 ≥98% (HPLC)		 1227158-85-1 25MG ￥45500 2023-06-01 購入

BAY 87-2243 化学特性,用途語,生産方法

酵素阻害剤

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.

BAY 87-2243 上流と下流の製品情報

原材料

1-エチルオキシ-1-(トリメチルシリルオキシ)シクロプロパン

準備製品

BAY 87-2243 生産企業

Global( 92)Suppliers
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 masar@topule.com China 8474 58

  スペクトルデータ(1HNMR)

BAY 87-2243(1227158-85-1)1HNMR

1227158-85-1()キーワード:

AG1296 ボリノスタット (1R,2E,6S,10E,11aS,13S,14aR)-1,6,7,8,9,11a,12,13,14,14a-デカヒドロ-1,13-ジヒドロキシ-6-メチル-4H-シクロペンタ[f]オキサシクロトリデシン-4-オン BORTEZOMIB (VELCADE) Y-27632二塩酸塩 MK-2206 りんご酸スニチニブ 4-[(2S)-2-アミノ-2-カルボキシエチル]-N,N-ビス(2-クロロエチル)ベンゼンアミンオキシド/塩酸,(1:2) ルキソリチニブ
  • 1227158-85-1
  • 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
  • BAY 87-2243 USP/EP/BP
  • 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]-
  • 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]pyridin-2-yl}piperazine
  • 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
  • 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
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