1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. Rogaratinib

Rogaratinib (Synonyms: BAY1163877)

目录号: HY-100019 纯度: 99.86%
产品使用指南

Rogaratinib (BAY1163877) 是一种有效且有选择性的成纤维细胞生长因子受体 (FGFR) 抑制剂。

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Rogaratinib Chemical Structure

Rogaratinib Chemical Structure

CAS No. : 1443530-05-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4619
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1 mg ¥1500
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5 mg ¥4500
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10 mg ¥6500
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50 mg ¥19500
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100 mg ¥29500
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200 mg   询价  
500 mg   询价  

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Top Publications Citing Use of Products

    Rogaratinib purchased from MCE. Usage Cited in: IOP Conf Ser Mater Sci Eng. 562 (2019) 012128.

    Effects of BAY1163877 on the Expression of p-FGFR1/FGFR1 and p-STAT3/STAT3 Protein in Breast Cancer Cell Lines MDA-MB-231 and MCF-7 are showed.

    查看 FGFR 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor.

    IC50 & Target[1]

    FGFR1

     

    FGFR2

     

    FGFR3

     

    FGFR4

     

    体外研究
    (In Vitro)

    Of the 24 cell lines, 2 FGFR1-amplified lung cancer (LC) cell lines, H1581 and DMS114, show extreme sensitivity to Rogaratinib (BAY1163877) (GI50 values ranging from 36 to 244 nM). Treatment with Rogaratinib results in a significant decrease in colonies formed by H1581P cells, but not by H1581AR and BR cells. Ectopic expression of Met significantly induces resistance to Rogaratinib in MTT assays. Met overexpression induces activation of downstream extracellular signal-regulated kinase 1/2 (ERK1/2) and AKT, which cannot be abrogated by Rogaratinib treatment[1].

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

    Clinical Trial
    分子量

    466.56

    Formula

    C23H26N6O3S

    CAS 号
    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 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 5 mg/mL (10.72 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1433 mL 10.7167 mL 21.4335 mL
    5 mM 0.4287 mL 2.1433 mL 4.2867 mL
    10 mM 0.2143 mL 1.0717 mL 2.1433 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: ≥ 0.56 mg/mL (1.20 mM); Clear solution

      此方案可获得 ≥ 0.56 mg/mL (1.20 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 5.6 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% (20% SBE-β-CD in saline)

      Solubility: ≥ 0.56 mg/mL (1.20 mM); Clear solution

      此方案可获得 ≥ 0.56 mg/mL (1.20 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 5.6 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 0.56 mg/mL (1.20 mM); Clear solution

      此方案可获得 ≥ 0.56 mg/mL (1.20 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 5.6 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    Cell Assay
    [1]

    Cells (3000 cells/well) are seeded on 96-well plates at 37°C. After overnight incubation, the cells are treated with Rogaratinib for 72 h. Then, MTT reagent [3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide] is added to each well and incubated for 4 h at 37°C. MTT solubilization solution/stop mix is added to each well, mixed, and the plates are incubated overnight at 37°C. After measuring the absorbance at 570 nm, the data are graphically displayed[1].

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

    参考文献

    纯度: 99.86%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    Rogaratinib
    目录号:
    HY-100019
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