Imatinib Mesylate
Other Name:Glivec;gleevec;imatinib methanesulfonate;imatinib mesilate;Imatinibmesylate;4-[(4-methylpiperazin-1-yl)methyl]-n-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide methanesulfonate;4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide monomethanesulfonate
CAS:220127-57-1
MF:C30H35N7O4S
MW:589.71
Assay:99%min
Appearence:White powder
Drug category:Anti tumor drug
Purpose:A tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL).
Imatinib mesylate is a tyrosine kinase inhibitor IC50 value of 100 nM, 100 nM, 600 nM for v-Abl, c-kit, PDGFR, respectively.
Imatinib Mesylate is a specific tyrosine kinase (abl, c-kit, and PDGFR) inhibitor and is reported to sensitize cells to radio- or chemo-therapy. When tested with Y-79 and WERI-RB-1 Rb cell lines, imatinib mesylate treatment decreased the cell proliferation and invasion with the concentration of 10 μM . In osteoblast cells, administration of imatinib mesylate decreased osteoclast development via stimulating differentiation, inhibiting proliferation and survival .
In dog model with mast cell tumor, administration of imatinib mesylate at a dose of 10 mg/kg daily for 1-9 weeks reduced tumor growth via inhibiting tyrosine kinase .
Cells were stimulated with allogeneic mature DCs or PHA in the presence of imatinib mesylate. The drug inhibited T-cell proliferation as a function of concentration. The effects were significant at 0.5 μM imatinib mesylate for the cells stimulated by DCs and at 1.0 μM imatinib mesylate for the cells stimulated with PHA. The IC50 values for imatinib mesylate-inhibited T-cell proliferation stimulated by DCs and PHA were 3.9 μM and 2.9 μM, respectively..
A tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL)
Imatinib Mesylate is orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively. Imatinib also known as Gleevec, Glivec, CGP-57148B, STI-571 & Imatinib
Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.
echinocandin antifungal, active against infections with Aspergillus and Candida, inhibits cell wall synthesis
imatinib Dosage
Starting dose: in patients with chronic myelogenous leukemia radically increasing stage and accelerating stage, imatinib mesylate in the recommended dose of 600 mg/day;
Chronic-phase of interferon treatment failure, and cannot be removed surgically or metastatic malignant gastrointestinal stromal tumors (GIST) patients, and the recommended dose of 400 mg/day, both for once-daily oral, appropriate medication when eating, and drinking a glass of water, as long as effective, should be continued.