Imatinib, Methanesulfonate Salt (Imatinib Mesylate, Glamox, Gleevec, Glivec, CGP-57148B, STI-571, CAS 220127-57-1), >99%

LC Laboratories' Product Number I-5508 - Imatinib, Methanesulfonate Salt (Imatinib Mesylate, Glamox, Gleevec, Glivec, CGP-57148B, STI-571), >99% - for research use only. Imatinib inhibits bcr-abl tyrosine kinase activity, upon which some types of tumor cells depend for growth. Imatinib acts by binding to the ATP binding site of bcr-abl and competitively inhibiting its tyrosine kinase activity. Imatinib is selective for bcr-abl, but it also targets several other kinases (c-kit and PDGF-R). Imatinib also stimulates the entry of the bcr-abl tyrosine kinase into the nucleus, where it cannot perform its anti-apoptopic functions. Imatinib inhibits EOL-1 cell viability (IC50 = 0.5 nM), phosphorylation of a fusion protein (IC50 = 30 nM), and viability of BaF3 cells expressing Rhe-PDGFRα in the absence of IL-3 (IC50 = 0.17 nM). Inhibition of CSF-1R by imatinib is competitive with ATP, with a Ki value of 120 nM. The IC50 values for imatinib inhibition of KBM5 and KBM7 cell growth were about 0.48 and 0.24 µM, respectively, while the IC50 values for imatinib in KBM5-STI571R1.0 and KBM7-STI571R1.0 cells were about 6.40 and 3.30 µM, respectively. The calculated resistance indexes for imatinib were 13.3 for KBM5-STI571R1.0 cells and 13.8 for KBM7-STI571R1.0 cells. Imatinib is the active ingredient in the drug sold under the trade name Gleevec® in USA or Glivec in Europe and Australia. This drug has been approved in at least one country for use in patients with gastrointestinal stromal tumors, chronic myelogenous leukemia and a number of other malignancies.

• Supplier: LC Laboratories
• Product #: I-5508
• Sku #: I-5508_1g