Imatinib Mesylate-cancer research-TOKU-E

Detailed Description

Imatinib Mesylate is a tyrosine kinase inhibitor used primarily in leukemia research. Chronic Myeloid Leukemia (CML) cells contain a hybrid tyrosine kinase BCR/ABL that works to provide the cancer cell with ATP at an uncontrolled rate. Imatinib Mesylate inhibits this protein to slow cell growth and promote apoptosis.

Mechanism of Action

Imatinib Mesylate binds to the ATP binding site of the BCR/ABL tyrosine kinase. This enzyme is the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in chronic myeloid leukemia (CML).

Molecular Formula

C₂₉H₃₁N₇O•CH₃SO₃H

References

Goldman JM and Melo JV (2003) Chronic myeloid leukemia — Advances in biology and new approaches to treatment. New England J. of Med. 349(15):1451-1464

Marcucci B, Perrotti D, Caligiuri MA (2003) Understanding the molecular basis of Imatinib Mesylate therapy in chronic myelogenous leukemia and the related mechanisms of resistance. Clin. Cancer Res. 9(4):1248-1252

Mohamed AN, Pemberton P, Zonder J, Schiffer CA. The effect of imatinib mesylate on patients with Philadelphia chromosome-positive chronic myeloid leukemia with secondary chromosomal aberrations. Clin Cancer Res. 2003 Apr;9(4):1333-7. PMID: 12684401.