2. Metabolic Enzyme/Protease Apoptosis
  3. HIF/HIF Prolyl-Hydroxylase Ferroptosis
  4. BAY 87-2243

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。

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BAY 87-2243

BAY 87-2243 Chemical Structure

CAS No. : 1227158-85-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥989
In-stock
1 mg ￥342
In-stock
5 mg ￥855
In-stock
10 mg ￥1200
In-stock
25 mg ￥2180
In-stock
50 mg ￥3500
In-stock
100 mg ￥5800
In-stock
200 mg   询价  
500 mg   询价  

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Customer Review

BAY 87-2243 相关抗体

Top Publications Citing Use of Products

    BAY 87-2243 purchased from MCE. Usage Cited in: Radiother Oncol. 2015 Sep;116(3):431-7.  [Abstract]

    Radiation-induced Hif1α expression and blockage by BAY87-2243 or EGFR siRNA. A549 and FaDu cells are pretreated with BAY87-2243 or hypoxia and irradiated with 2 Gy. Six hours after irradiation, cells are lysed, and Western blotting is performed.

    查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

    查看所有亚型
    HIF-1α HIF

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

    IC50 & Target

    HIF-1α[1]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    G-361 IC50
    4.8 μM
    Compound: 38; BAY 87-2243
    Antiproliferative activity against human G-361 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay
    Antiproliferative activity against human G-361 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay
    		[PMID: 36332549]
    PC-3 IC50
    10 nM
    Compound: BAY 87-2243
    Inhibition of complex-I-dependent oxygen consumption in mitochondria of human PC-3 cells by luxcel-dye staining based MitoXpress method
    Inhibition of complex-I-dependent oxygen consumption in mitochondria of human PC-3 cells by luxcel-dye staining based MitoXpress method
    		[PMID: 34982568]
    SK-MEL-28 IC50
    2.4 μM
    Compound: 38; BAY 87-2243
    Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay
    Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay
    		[PMID: 36332549]
    体外研究
    (In Vitro)

    BAY 87-2243 抑制荧光素酶活性，IC50 为约 0.7 nM；在 HCT116luc 细胞中抑制 HIF 靶基因 CA9 的蛋白表达，IC50 为约 2 nM；通过氧敏荧光染料 LUX-MitoXpress 测定，抑制线粒体氧气消耗的 IC50 为约 10 nM；还抑制核 HIF-1α 蛋白表达。在 HIF-1α 表达相关实验中，显著降低低氧分数和坏死分数，同时相对血管面积和灌注血管未变化[1]. [2].

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

    BAY 87-2243 相关抗体:
    体内研究
    (In Vivo)

    裸鼠皮下接种 H460 细胞，肿瘤形成后，通过每日口服管饲法用 BAY 87-2243(0.5、1、2 和 4 mg/kg)治疗 3 周。BAY 87-2243 剂量依赖性地降低肿瘤重量，这与 HIF-1 靶基因 CA9、ANGPTL4 和 EGLN3 的 mRNA 表达水平剂量依赖性降低一致，而体内化合物治疗不影响缺氧不敏感的 EGLN2 基因和 HIF-1α 本身的 mRNA 表达水平[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    525.53

    Formula

    C26H26F3N7O2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 20 mg/mL (38.06 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    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
    查看完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.40%

    COA (282 KB) HNMR (260 KB) RP-HPLC (224 KB) LCMS (102 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    Luciferase activity is given in % of DMSO-treated cells. To evaluate the cytotoxicity of BAY 87-2243, 2.000 cells of the respective cell lines are seeded in 96-well plates and cultured in the appropriate growth medium containing 10% FCS. BAY 87-2243 at various concentrations is added at 24 h after seeding for additional 48 h and cell viability is determined using Cell Titer Glow Assay[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Tumor xenograft experiment is carried out on female immune-deficient, athymic NMRI nude mice, aged 7-9 weeks, weighing 20-25 g. The lung carcinoma xenograft mouse model is established by subcutaneous injection into the right flank with 0.1 mL H460 tumor cells (1.5×106) mixed 1:1 with Matrigel. Mice are randomized into control and BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) groups when tumors reach a size of more than 40 mm2. Body weight is monitored as a measure for treatment-related, acute toxicity. Tumor area (measured by caliper) or tumor weight (measured when mice are sacrificed 21 days after cell injection) is calculated by the formula 100-100×(tumor weight/area of treatment group)/(tumor weight/area of vehicle group). Tumor Statistical analysis is performed using the one-way analysis of variance.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    BAY 87-2243 相关分类

    完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9028 mL 9.5142 mL 19.0284 mL 47.5710 mL
    5 mM 0.3806 mL 1.9028 mL 3.8057 mL 9.5142 mL
    10 mM 0.1903 mL 0.9514 mL 1.9028 mL 4.7571 mL
    15 mM 0.1269 mL 0.6343 mL 1.2686 mL 3.1714 mL
    20 mM 0.0951 mL 0.4757 mL 0.9514 mL 2.3786 mL
    25 mM 0.0761 mL 0.3806 mL 0.7611 mL 1.9028 mL
    30 mM 0.0634 mL 0.3171 mL 0.6343 mL 1.5857 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    BAY 87-22431227158-85-1HIF/HIF Prolyl-HydroxylaseFerroptosisHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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    目录号：
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