Imatinib
| CAS No. | 152459-95-5 | Cat. No. | BCP01542 |
| Name | Imatinib | ||
| Synonyms | STI571;Glivec;STI-571;STI 571;STI571; | ||
| Formula | C29H31N7O | M. Wt | 493.6 |
| Description | In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively.Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively. A recent study shows that Imatinib has the potential to exert its antileukemia effects in chronic myelogenous leukemia by down-regulating hERG1 K(+) channels, which are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis. | ||
| Pathways | Angiogenesis/Protein Tyrosine Kinase | ||
| Targets | Src/Bcr Abl PDGFR c Kit | ||
Structure
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