Description
Imatinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit.1 It inhibits ligand-stimulated autophosphorylation of PDGFR and c-Kit (IC50s = ~0.3 and ~0.1 μM, respectively).1,2 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.1,3 It prolongs survival in a mouse model of chronic myeloid leukemia when administered at a dose of 100 mg/kg twice per day.4 Formulations containing imatinib have been used in the treatment of various cancers.WARNING This product is not for human or veterinary use.
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