SML2384
BAY 87-2243
≥98% (HPLC)
别名:
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
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About This Item
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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
CC1=CC(C2=NC(C3=CC=C(OC(F)(F)F)C=C3)=NO2)=NN1CC4=CC(N5CCN(C6CC6)CC5)=NC=C4
InChI
1S/C26H26F3N7O2/c1-17-14-22(25-31-24(33-38-25)19-2-6-21(7-3-19)37-26(27,28)29)32-36(17)16-18-8-9-30-23(15-18)35-12-10-34(11-13-35)20-4-5-20/h2-3,6-9,14-15,20H,4-5,10-13,16H2,1H3
InChI 密鑰
CDJNNOJINJAXPV-UHFFFAOYSA-N
生化／生理作用
BAY 87-2243 has a therapeutic effect on ferroptosis‐based 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).
Highly potent and selective mitochondrial complex I inhibitor that prevents hypoxia-induced HIF-1 activation both in vitro and in vivo.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Peter Ellinghaus et al.
Cancer medicine, 2(5), 611-624 (2014-01-10)
The activation of the transcription factor hypoxia-inducible factor-1 (HIF-1) plays an essential role in tumor development, tumor progression, and resistance to chemo- and radiotherapy. In order to identify compounds targeting the HIF pathway, a small molecule library was screened using
Gertrud Knoll et al.
Oncotarget, 7(27), 41488-41504 (2016-05-12)
The capacity of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) to selectively induce cell death in malignant cells triggered numerous attempts for therapeutic exploitation. In clinical trials, however, TRAIL did not live up to the expectations, as tumors exhibit high rates
PKM2 promotes tumor angiogenesis by regulating HIF-1 alpha through NF-kappaB activation
Azoitei N, et al.
Molecular Cancer, 15(1), 3-3 (2016)
Qingjie Zhao et al.
Frontiers in immunology, 8, 637-637 (2017-06-18)
As important effector cells in inflammation, macrophages can be functionally polarized into either inflammatory M1 or alternatively activated anti-inflammatory M2 phenotype depending on surroundings. The key roles of glycolysis in M1 macrophage polarization have been well defined. However, the relationship
Emerging strategies of cancer therapy based on ferroptosis
Shen z, et al.
Advanced Materials, 30(12), 1704007-1704007 (2018)
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