Pricing updated 2019-06-26. Prices are subject to change without notice.
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.
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Heinrich, M.C., Griffith, D.J., Druker, B.J., et al. Inhibition of c-
Buchdunger, E., Zimmermann, J., Mett, H., et al. Inhibition of the Abl protein-
3. Wolff, N.C., Veach, D.R., Tong, W.P., et al. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia Blood 105(10), 3995-4003 (2005).