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CAS No.: 1227158-85-1

BAY 87-2243 Catalog No. CSN17588

Synonyms: BAY 87-2243

BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced HIF-1 activation.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The response of mammalian cells to hypoxia is mediated by a family of transcription factors known as HIF (hypoxia-inducible factors). The subunits of HIF, HIF-1αand HIF-2αare structurally similar and can be degraded rapidly under normoxia through a posttranslational process involving proline hydroxylation in an oxygen dependent manner targeting HIF proteins to the VHL ubiquitination complex for final degradation by the proteasome system. BAY 87-2243 is a HIF-1 inhibitor with IC50 value of 0.7nM (measure by luciferase reporter gene). Treatment with BAY 87-2243 (1-100nM) for 16h inhibited HIF-1α and HIF-2αprotein accumulation in a dose-dependent manner in H460 cells under hypoxia (1% pO₂) but hypoxia mimetics. Consistent with that, expression of HIF target genes CA9, ADM and ANGPTL4 was suppressed dose-dependently in hypoxic lung cancer cells treated with BAY 87-2243 (10-1000nM) for 16h. The activity of BAY 87-2243 against HIF-1 protein and its target gene depends on intact VHL protein and PHD activity. BAY 87-2243 also functioned as a mitochondrial complex I inhibitor and inhibited mitochondrial oxygen consumption measured by using the oxygen sensitive fluorescence dye LUX-MitoXpress with an IC50 value of ~10 nM. Once daily oral treatment with BAY 87-2243 (0.5, 1.0, 2.0, and 4.0 mg/kg for 21 days) could inhibit tumor growth dose-dependently in nude mice bearing established H460 human tumor xenografts^[1].
动物研究
剂量
Nude Mice: 9 mg/kg^[2] (p.o.); 0.5 mg/k - 4 mg/kg^[1] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Nude Mice: 9 mg/kg^[2] (p.o.); 0.5 mg/k - 4 mg/kg^[1] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01297530	Neoplasms	Phase 1	Terminated	-	Germany ... more >> Freiburg, Baden-Württemberg, Germany, 79106 Norway Oslo, Norway, 0424 United Kingdom Sutton, Surrey, United Kingdom, SM2 5PT Collapse <<

参考文献

[1] Ellinghaus P, Heisler I, et al. 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. 2013;2(5):611-24.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9028 mL
- 9.5142 mL
- 19.0284 mL
- 5 mM
- 0.3806 mL
- 1.9028 mL
- 3.8057 mL
- 10 mM
- 0.1903 mL
- 0.9514 mL
- 1.9028 mL

技术信息

CAS号

1227158-85-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H26F3N7O2

运输

蓝冰

分子量

525.53

别名

BAY 87-2243

溶解度

DMSO	18.0 mg/mL (34.3 mM) warming
Water	Insoluble
Ethanol	8.0 mg/mL (15.2 mM) warming

动物实验配方

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