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BAY 87-2243

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Chemical Structure| 1227158-85-1 同义名 : -
CAS号 : 1227158-85-1
货号 : A633112
分子式 : C26H26F3N7O2
纯度 : 99%+
分子量 : 525.526
MDL号 : MFCD28143915
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(47.57 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • HIF
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.51mL

1.90mL

0.95mL

19.03mL

3.81mL

1.90mL
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.