Product Description
EGFR (L858R) is an oncogenic mutant form of the epidermal growth factor receptor (EGFR), a member of the receptor tyrosine kinase (RTK) family that plays a pivotal role in cell proliferation, survival, differentiation, and tumorigenesis. The L858R mutation, located in the kinase domain of EGFR, results in constitutive activation of the receptor in a ligand-independent manner, leading to sustained downstream signaling through pathways such as MAPK, PI3K/AKT, and STAT. This activating mutation is one of the most common alterations identified in non‑small cell lung cancer (NSCLC) and serves as a critical driver of oncogenesis. Beyond its role in tumor initiation and progression, dysregulation of EGFR (L858R) signaling is closely associated with sensitivity to first‑ and second‑generation EGFR tyrosine kinase inhibitors (such as erlotinib and gefitinib), while also contributing to acquired resistance mechanisms, making it a highly validated target for cancer therapy and precision medicine.
Screeningbio’s EGFR (L858R) Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying EGFR (L858R) 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: EGFR (L858R) 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 EGFR (L858R) kinase.
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