85-1500-95　Imatinib, Methanesulfonate Salt (STI-571, CGP-57148B) 5g　CAS No:220127-57-1　G2035-20

特徴

• A tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). 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). (1)
• Imatinib also stimulates the entry of the bcr-abl tyrosine kinase into the nucleus, where it cannot perform its anti-apoptopic functions. (2)
• 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). (3)
• Inhibition of CSF-1R by imatinib is competitive with ATP, with a Ki value of 120nM. (4)
• 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 3.30uM, respectively. (The data were from figure 2 but we found several errors in the figure. The correct data cannot be determined without further information). The calculated resistance indexes for imatinib were 13.3 for KBM5-STI571R1.0 cells and 13.8 for KBM7-STI571R1.0 cells. (5)
• 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. NOTE: The imatinib sold by LC Laboratories is NOT Gleevec® or Glivec, and is NOT for human use.
• Solubility:Soluble in DMSO at 100mg/ml. Very poorly soluble in ethanol; soluble in water at 200mg/ml.; buffers, serum or other additives may increase or decrease the aqueous solubility.
• Elemental Analysis:Calculated:C: 61.10%H: 5.98%N: 16.63%S: 5.44%
• Storage and Stability:May be stored at RT for short-term only. Long-term storage is recommended at -20°C for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap.