您的位置:首页 > 产品中心 > 1227158-85-1, BAY 87-2243
BAY 87-2243
产品价格查看更多规格...
产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
4086006 | 5 MG | 958 | |||
4086006 | 25 MG | 3360 |
产品别名
1227158-85-1
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
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
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C26H26F3N7O2 |
Molecular weight | 525.53 |
MDL number | MFCD28143915 |
Biochem/physiol Actions【生化/生理作用】 | BAY 87-2243 has a therapeutic effect on ferroptosis‐ased cancer, hypoxic pancreatic cancer cells. BAY 87-2243 is an orally active oxidative phosphorylation (OxPhos) inhibitor that potently suppresses hypoxia-induced HIF-1 activation (IC50 = 0.7 nM by HCT-116-based reporter assay; 24 h 1% O2) by selectively targeting mitochondrial complex I (IC50 = 10 nM using mitochondria from PC3; no inhibition of complex III), exhibiting antiproliferation activity in cancer cultures only in the absence of glucose (IC50 ∼3 nM in H460 cultures with 10 mM galactose or lactate, >10 μM with 10 mM glucose). BAY 87-2243 selectively inhibits hypoxia-induced, but not hypoxia-independent, HIF-1α & HIF-2α upregulation and HIF-1 target genes expression in cultures (IC50 ≤10 nM/ADM, ANGPTL4, CA9 mRNA in H460 cells; IC50 = 2 nM/carbonic anhydrase 9 (CA9) protein in HCT116 cells) and effectively suppresses H460 xenograft tumor growth in mice via daily oral admiminstration in vivo (ED50 ∼2 mg/kg). |
产品性质
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
color【颜色】 | white to beige |
solubility【溶解性】 | DMSO: 2 mg/mL, clear |
storage temp.【储存温度】 | 2-8℃ |
SMILES string | CC1=CC(C2=NC(C3=CC=C(OC(F)(F)F)C=C3)=NO2)=NN1CC4=CC(N5CCN(C6CC6)CC5)=NC=C4 |
安全信息
Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
WGK | WGK 3 |