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Background: PDGFRα (platelet-derived growth factor receptor A), also known as CD140a, is one of the isoforms of the tyrosine kinase receptor for PDGF (platelet-derived growth factor), belonging to the family of RTK class III family of proteins. Binding of PDGF induces receptor dimerization and trans-phosphorylation, which leads to the recruitment of signaling and adaptor proteins and activation of downstream signaling cascades, such as the PI3K (phosphoinositide 3-kinase)-mTOR (mammalian target of rapamycin). It has been implicated in the regulation of cell growth and survival, apoptosis, and differentiation. It has been identified as a potential target in eosinophilic leukemia cancer, inflammatory breast cancer, and gastrointestinal stromal tumors (GIST). GIST is one of the most common mesenchymal cancers in the gastrointestinal tract, with 10-15% of the mutations leading to constitutively active PDGFRα. D842Y is a mutation in exon 18, and differently from other D842 mutations, D842Y is not imatinib resistant. The study of PDGFRα and the development of new inhibitors may benefit the cancer therapy field.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ PDGFRα (D842Y) Kinase Assay Kit is designed to measure PDGFRα (platelet-derived growth factor receptor A) (D842Y) tyrosine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified PDGFRα (D842Y) (amino acids 550-1089(end)), kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Supplied As: The assay kit comes in a convenient 96-well format, with enough purified PDGFRα (D842Y) (amino acids 550-1089(end)), kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Uniprot: P16234
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: Guerit E., et al., 2021 Cell Mol Life Sci 78(8):3867-3881.Sun Y., et al., 2022 Front Oncol. 12: 927587.