产品描述:
Imatinib-d3 is intended for use as an internal standard for the quantification of imatinib (Item No. 13139) by GC- or LC-MS. Imatinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit.{47196} It inhibits ligand-stimulated autophosphorylation of PDGFR and c-Kit (IC50s = ~0.3 and ~0.1 μM, respectively).{47196,47197} Imatinib inhibits the proliferation of Bcr-Abl-dependent R10(–) cells (IC50s = ~35-40 nM) and HMC-1 cells expressing constitutively active c-Kit in a concentration-dependent manner.{47196, 20180} It prolongs survival in a mouse model of chronic myeloid leukemia when administered at a dose of 100 mg/kg twice per day.{20177} Imatinib (25 and 50 µM) also inhibits the replication of Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in Vero E6 cells.{57353} It reduces viral titers in Vero cells infected with infectious bronchitis virus (IBV), a coronavirus, when used at a concentration of 10 µM via inhibition of IBV surface glycoprotein protein-induced syncytia formation and virus-cell fusion.{45828} Formulations containing imatinib have been used in the treatment of various cancers.