IMATINIB MESYLATE (C005B-312644)

Application

Imatinib mesylate (IM) has been used:

• in sulforhodamine B cell viability assay to study its effect on CD34⁺ or CD38^- and CD34⁺ or CD38⁺ cells
• as an abelson1 (ABL1) kinase inhibitor
• in circular dichroism analysis to study the effect of IM binding on the secondary structure of the human transferrins

Biochem/physiol Actions

Imatinib mesylate is a tyrosine kinase inhibitor with antineoplastic activity. Imatinib is a potent inhibitor of the Bcr-Abl kinase encoded by the bcr-abl oncogene as well as receptor tyrosine kinases encoded by c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Imatinib mesylate inhibition of Bcr-Abl tyrosine kinase created by the Philadelphia chromosome abnormality found in CML decreases proliferation and enhances apoptosis in leukemias CML and ALL. Inhibition of c-kit tyrosine activity inhibits mast-cell and cellular proliferation in those diseases overexpressing c-kit such as gastrointestinal stromal tumor (GIST).

Features and Benefits

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Other Notes

Imatinib has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the Imatinib probe summary on the Chemical Probes Portal website.