BAY 87-2243|cas:1227158-85-1|西域试剂

BAY 87-2243,99.41%

产品编号：Bellancom-15836| CAS NO：1227158-85-1| 分子式：C₂₆H₂₆F₃N₇O₂| 分子量：525.53

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货号	价格	库存与货期
Bellancom-15836	￥855.00	杭州北京（现货）
Bellancom-15836	￥1200.00	杭州北京（现货）
Bellancom-15836	￥5200.00	杭州北京（现货）
Bellancom-15836	￥8320.00	杭州北京（现货）

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BAY 87-2243

产品介绍

BAY 87-2243 是一种有效的选择性的缺氧诱导因子-1 (HIF-1) 抑制剂。

生物活性

BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.

体外研究

BAY 87-2243 inhibits luciferase activity with a calculated IC₅₀ value of ~0.7 nM. Hypoxic induction of the HIF target gene CA9 on protein level in HCT116luc cells is inhibited by BAY 87-2243 with an IC₅₀ value of ~2 nM. BAY 87-2243 inhibits mitochondrial oxygen consumption measured by using the oxygen sensitive fluorescence dye LUX-MitoXpress with an IC₅₀ value of ~10 nM. BAY-87-2243 inhibits nuclear HIF-1α protein expression. Administration of BAY-87-2243 for about 18 days significantly reduces HIF-1α protein expression as well as pimonidazole hypoxic fraction (pHF) (mean 2.4% (BAY-87-2243) vs. 17.6% (carrier), p<0.0001), and necrotic fraction (NF) (mean 9% vs. 35.6%, p=0.0002), whereas relative vascular area (RVA) and perfused vessels (PF) remained unchanged.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Nude mice are inoculated with H460 cells subcutaneously and after tumors have been established, animals are treated with BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) for 3 weeks by daily oral gavage. BAY 87-2243 reduced tumor weight dose dependently in line with a dose-dependent reduction of the mRNA expression levels of the HIF-1 target genes CA9, ANGPTL4, and EGLN3, whereas the mRNA expression levels of hypoxia-insensitive EGLN2 gene and of HIF-1α itself are not affected by compound treatment in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (47.57 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.76 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.76 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。