2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR4-IN-24

FGFR4-IN-24 是一种具有选择性的不可逆共价 FGFR4 抑制剂 (IC50 = 1.2 nM)。FGFR4-IN-24 对其他三种 FGFR 家族激酶 (FGFR1-3) 的活性较弱。FGFR4-IN-24 可抑制 FGF19/FGFR4 信号通路，有效抑制 HuH-7 肝癌细胞系的增殖 (GI50 = 17 nM)。FGFR4-IN-24 在 HuH-7 小鼠异种移植模型中表现出显著的抗肿瘤活性。FGFR4-IN-24 可用于肝细胞癌的研究。

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FGFR4-IN-24

FGFR4-IN-24 Chemical Structure

CAS No. : 3053546-73-6

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FGFR4-IN-24 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR4-IN-24 is a selective irreversible covalent FGFR4 inhibitor (IC50 = 1.2 nM). FGFR4-IN-24 shows much weaker activity against the other three FGFR family kinases (FGFR1-3). FGFR4-IN-24 inhibits the FGF19/FGFR4 signaling pathway, effectively suppressing the proliferation of the HuH-7 HCC cell line (GI50 = 17 nM). FGFR4-IN-24 exhibits significant antitumor activity in a HuH-7 mouse xenograft model. FGFR4-IN-24 can be used for the research of hepatocellular carcinoma[1].

IC50 & Target[1]

FGFR4

1.2 nM (IC50)

体外研究
(In Vitro)

FGFR4-IN-24 (Compound 10v) (3 nmol/L, 0-30 分钟) 的表观抑制活性随预孵育时间的延长而增强，这与其共价修饰 FGFR4 的能力相符[1]。
FGFR4-IN-24 (kinact/KI = 4.8 × 105 M-1s-1) 表现出更强的效力，这主要是由于其与 FGFR4 激酶的结合更紧密 (KI = 0.62 nM)，这种结合模式增强了非共价亲和力[1]。
FGFR4-IN-24 (72 小时) 抑制 HuH-7 细胞系的增殖 (IC50 = 1.2 nM, GI50 = 17 nM)[1]。
FGFR4-IN-24 (1 μM) 对 FGFR4 表现出显著的抑制作用 (79%)，且具有高选择性[1]。
FGFR4-IN-24 (1-1000 nM, 2 小时) 抑制 FGFR4 底物 FRS2α 的磷酸化，并降低 HuH-7 细胞中 ERK 的磷酸化水平[1]。

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

FGFR4-IN-24 相关抗体:

Cell Viability Assay[1]

Cell Line: HuH-7 cells
Concentration:
Incubation Time: 72 h
Result: Induced a growth inhibition 50% (GI50) of 17 nM.

Western Blot Analysis[1]

Cell Line: HuH-7 cells
Concentration: 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 2 h
Result: Inhibited almost completely the phosphorylation of FRS2α at 100 nM.
Reduced the phosphorylation levels of ERK.
Maintained the inhibition of FRS2α and ERK phosphorylation at 300 nM even after extensive washing with phosphate-buffered saline (PBS) (HY-K3005).
体内研究
(In Vivo)

FGFR4-IN-24 (Compound 10v) (25, 50 mg/kg，腹腔注射，每天两次，持续 21 天) 以剂量依赖的方式抑制 HuH-7 异种移植小鼠模型肿瘤生长并维持体重[1]。

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

Animal Model: HuH-7 xenograft mouse model in female BALB/c nude mice (4 weeks)[1]
Dosage: 25, 50 mg/kg
Administration: Intraperitoneal administration (i.p.), twice daily for 21 days
Result: Significantly inhibited tumor growth at 25 mg/kg, with a tumor growth inhibition (TGI) ratio of 85%.
Caused tumor regression at 50 mg/kg, with a TGI ratio of 114%.
Induced no significant reduction in body weight.
分子量

483.49

Formula

C27H22FN5O3
CAS 号
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

FGFR4-IN-24 相关分类

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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:

FGFR4-IN-243053546-73-6FGFRFibroblast growth factor receptorFibroblast growth factor receptor 4Irreversible covalent inhibitorHepatocellular carcinomaInhibitorinhibitorinhibit

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