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Imatinib mesylate can inhibit Bcr-Abl tyrosine kinase in vitro and in vivo, selectively inhibit proliferation and induce apoptosis in Bcr-Abl positive cell lines, Ph chromosome-positive chronic myelogenous leukemia and acute lymphoblastic leukemia patients. In addition, imatinib mesylate also inhibits tyrosine kinases of platelet-derived growth factor (PDGF) receptors, stem cell factor (SCF) receptors, and c-Kit receptors, thereby inhibiting PDGF and stem cell factor-mediated cell behavior. Some patients develop resistance through different mechanisms.
Uses of Imatinib mesylate.
It is used to treat patients with chronic myelogenous leukemia (CML) in the acute phase, accelerated phase or chronic phase after the failure of alpha-interferon therapy. Patients with malignant gastrointestinal stromal tumors (GIST) that cannot be resected or metastasized.
In vitro study of Imatinib mesylate.
In vitro assay of tyrosine and serine/threonine protein kinases showed that Imatinib effectively inhibited V-Abl tyrosine kinase and PDGFR with IC50 of 0.6μM and 0.1μM, respectively. Imatinib inhibits wild-type c-kit kinase activity in SLF-dependent activation with an IC50 of about 0.1μM, which is similar to the concentration required to inhibit PDGFR. Imatinib showed inhibitory effects on human bronchial cancer cell line NCI-H727 and human pancreatic cancer cell line BON-1 with IC50 of 32.4μM and 32.8μM, respectively. A recent study showed that Imatinib exerts anti-leukemia effects in chronic myelogenous leukemia by down-regulating the hERG1K(+) channel, which is highly expressed in leukemia cells and appears to favor leukemia.
Product method of Bulk Imatinib mesylate Powder.
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