Product Description
MET (M1250T), also known as c-Met (M1250T) or HGFR (M1250T), is a gain-of-function mutant variant of the MET receptor tyrosine kinase (RTK family) that plays a pivotal role in constitutive activation of downstream signaling pathways, driving aberrant cell proliferation, survival, migration, and epithelial-mesenchymal transition (EMT), as well as oncogenic transformation and therapeutic resistance. The M1250T mutation, located in the kinase domain of MET, leads to ligand-independent hyperactivation of the receptor, resulting in sustained phosphorylation and downstream activation of the PI3K/AKT, RAS/MAPK, STAT3, and Src/FAK pathways, thereby promoting tumor aggressiveness and metastasis. Beyond its role in normal MET signaling, dysregulation of MET (M1250T) signaling—through this activating mutation—is closely associated with multiple cancers (including hereditary papillary renal cell carcinoma, gastric cancer, non-small cell lung cancer, and hepatocellular carcinoma), as well as with acquired resistance to MET-targeted therapies (e.g., crizotinib), making MET (M1250T) a highly validated target for precision cancer therapy and drug discovery (particularly for developing next-generation MET inhibitors).
Screeningbio’s MET (M1250T) Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying MET (M1250T) 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: MET (M1250T) 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 MET (M1250T) kinase.
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