
Product Description
FGFR4 (Fibroblast growth factor receptor 4), also known as CD334, is a member of the receptor tyrosine kinase (RTK) family that plays a pivotal role in myogenesis, bile acid metabolism, glucose homeostasis, and cell proliferation, differentiation, and survival. FGFR4 binds with high affinity to ligands such as FGF19 (its primary ligand), as well as FGF1 and FGF2, leading to activation of downstream signaling pathways including RAS-MAPK, PI3K-AKT, and STAT3. Beyond its role in normal metabolic regulation and development, dysregulation of FGFR4 signaling—through gene amplification, overexpression, or activating mutations (e.g., V550E/L in the kinase domain)—is closely associated with hepatocellular carcinoma, rhabdomyosarcoma, breast cancer, prostate cancer, and colon cancer, where it promotes tumor growth, metastasis, and drug resistance, making it a highly validated target for cancer therapy and drug discovery.
Screeningbio’s FGFR4 Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying FGFR4 kinase activity and evaluating the potency of tyrosine kinase inhibitors (TKIs).
This kit utilizes the ADP-Glo Kinase Assay platform, a luminescent technology that measures the amount of ADP produced during the kinase reaction.
The assay is performed in two distinct steps:
Kinase Reaction: FGFR4 catalyzes the transfer of a phosphate group from ATP to a specific substrate, resulting in the production of phosphorylated substrate and ADP.
ADP-Glo™ Reagent Addition: After the kinase reaction, the ADP-Glo™ Reagent is added to terminate the reaction and deplete any remaining unreacted ATP.
Kinase Detection: The Kinase Detection Reagent is added to simultaneously convert the produced ADP back into ATP, which is then used by luciferase to generate a luminescent signal.
The light intensity produced is directly proportional to the ADP concentration and, consequently, to the enzymatic activity of the FGFR4 kinase.
Data
![TKs Kinase Inhibition Assay. Staurosporine was titrated using established assay protocol. Non-linear regression was used to plot RLU signal vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.](https://static.wixstatic.com/media/cbf7de_8ee1a450ed4645c981ba35f69ff405ea~mv2.png/v1/fill/w_49,h_45,al_c,q_85,usm_0.66_1.00_0.01,blur_2,enc_auto/cbf7de_8ee1a450ed4645c981ba35f69ff405ea~mv2.png)
