Imatinib Mesylate 152459-95-5
220127-57-1
Imatinib Mesylate, a tyrosine kinase inhibitor, is considered to be one of the first clinically useful agents in a new class of cancer agents called signal transduction inhibitors (STIs). STIs interfere with intracellular signaling pathways that have been implicated in the development of malignancies. Imatinib Mesylate inhibits the bcr-abl tyrosine protein kinase found in chronic myelogenous leukemia (CML). The use of Imatinib Mesylate in the treatment of CML represents a new advance in the treatment of CML. Imatinib Mesylate is active in all phases (chronic, accelerated, or blastic) of CML with high hematologic response rates and cytogenetic response rates.
Imatinib Mesylate's innovator is Novartis-Global and appears world-wide under the brand names: Gleevec and Glivec.
Imatinib Mesylate is a protein tyrosine kinase inhibitor. Inhibition of the bcr-abl tyrosine kinase results in inhibition of proliferation and induces apoptosis in bcr-able positive cell lines and in fresh leukemic cells from Philadelphia chromosome positive chronic myelogenous leukemia. Protein tyrosine kinases catalyze the transfer of phosphate from adenosine triphosphate (ATP) to the hydroxyl group of a tyrosine residue in the protein substrate. Imatinib Mesylate competitively inhibits the ATP binding site on Abl, PDGF, SCF, and c-Kit tyrosine kinases and inhibits PDGF- and SCF-mediated cellular events.
The resultant fusion protein, bcr-abl, is a constitutively active tyrosine kinase that is responsible for the development of CML. Imatinib Mesylate causes growth arrest or apoptosis in cells that express bcr-abl but does not affect normal cells.
Imatinib Mesylate appears in the following formulation and dosage:
Tablets: 100mg and 400mg
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| Imatinib Mesylate CAS number: | 152459-95-5 220127-57-1 |
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| Formula: | C29H31N7O, CH4O3S |
| Molecular mass: | 589.7 g/mol |
| Imatinib Mesylate Assay/Purity: | Typically NLT 98% |
