1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. FGFR4-IN-19

FGFR4-IN-19 (compound 8B) 是一种有效的共价成纤维细胞生长因子受体4 (FGFR4) 抑制剂(IC50=1.2 nM)。 FGFR4-IN-19 通过共价靶向 FGFR4 激酶结构域中罕见的半胱氨酸 (C552),实现了高效率和同型选择性。 FGFR4-IN-19 可用于肝细胞癌 (HCC) 的研究。

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FGFR4-IN-19 Chemical Structure

FGFR4-IN-19 Chemical Structure

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Customer Review

查看 FGFR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR4-IN-19 (compound 8B) is a potent covalent fibroblast growth factor receptor 4 (FGFR4) inhibitor (IC50=1.2 nM). FGFR4-IN-19 achieves high efficiency and isotype selectivity by covalently targeting a rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 can be used for hepatocellular carcinoma (HCC) research[1].

IC50 & Target[1]

FGFR4

1.2 nM (IC50)

FGFR1

4370 nM (IC50)

FGFR2

490 nM (IC50)

FGFR3

>5000 nM (IC50)

体外研究
(In Vitro)

FGFR4-IN-19 对 FGFR1 (IC50=4.4 μM) 和 FGFR2 (IC50=490 nM) 的抑制活性较弱,其余 IC50 值均在 5 μM 以上。 FGFR4-IN-19 在 FGFR 家族中具有高度选择性[1]
FGFR4-IN-19 显示出有效的细胞 FGFR4 结合性 (EC50= 52±7 nM) 相比于 FGFR1-3 (IC50>10 μM)[1]
FGFR4-IN-19 (0.3 μM, 24 h) 表现出良好的抗增殖活性,可有效阻断 Hep3B 细胞中的 FRS2 磷酸化进程[1]

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

Western Blot Analysis[1]

Cell Line: Hep3B cells
Concentration: 0.3 μM
Incubation Time: 24 h
Result: Blocked effectively FRS2 phosphorylation.

Cell Proliferation Assay[1]

Cell Line: Hep3B cells
Concentration: 0.3 μM
Incubation Time: 24 h
Result: Had the lowest EC50 value of 5 nM.
分子量

506.73

Formula

C21H14Cl3N5O4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 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
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.

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产品名称:
FGFR4-IN-19
目录号:
HY-158248
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