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FGFR1 Kinase Assay

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Compound Test Services

CT-001

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Product Description


FGFR1 (Fibroblast growth factor receptor 1), also known as CD331, is a member of the receptor tyrosine kinase (RTK) family that plays a pivotal role in embryonic development, tissue repair, angiogenesis, and cell proliferation, differentiation, and migration. FGFR1 binds with high affinity to ligands such as FGF2 (basic FGF), FGF1 (acidic FGF), and other members of the FGF family, leading to activation of downstream signaling pathways including RAS-MAPK, PI3K-AKT, and PLCγ. Beyond its role in normal development and homeostasis, dysregulation of FGFR1 signaling—through gene amplification, activating mutations, chromosomal translocations (e.g., in 8p11 myeloproliferative syndrome), or aberrant expression—is closely associated with breast cancer, lung cancer, glioblastoma, prostate cancer, and skeletal disorders, making it a highly validated target for cancer therapy and drug discovery.


Screeningbio’s FGFR1 Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying FGFR1 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:

  1. Kinase Reaction: FGFR1 catalyzes the transfer of a phosphate group from ATP to a specific substrate, resulting in the production of phosphorylated substrate and ADP.

  2. ADP-Glo™ Reagent Addition: After the kinase reaction, the ADP-Glo™ Reagent is added to terminate the reaction and deplete any remaining unreacted ATP.

  3. 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 FGFR1 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.
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.


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