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Imatinib Mesylate

Cat. No. M1799

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Imatinib Mesylate Structure
Synonym:

Gleevec, Glivec, CGP-57148B, STI-571

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
100mg USD 35 In stock
500mg USD 90 In stock
1g USD 150 In stock
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Quality Control & Documentation
Biological Activity

Imatinib Mesylate, the mesylate salt of imatinib, is a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Inhibition of the bcr-abl TK results in decreased proliferation and enhanced apoptosis in malignant cells of Philadelphia-positive (Ph+) hematological malignancies such as CML and ALL; effects on c-kit TK activity inhibit mast-cell and cellular proliferation in those diseases overexpressing c-kit, such as mastocytosis and gastrointestinal stromal tumor (GIST).

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines T cells
Preparation method Cell proliferation assays. T cells, 1 × 10^5 in 200 μL/well of 96-well microtiter plates, were stimulated with DCs or phytohemagglutinin M (PHA-M; 10 μg/mL) or PDGF or both in a final volume of 0.2 mL/well. The cells were incubated with graded concentrations of imatinib mesylate, incubated for 4 days, pulsed with 2.0 μCi (0.074 MBq) tritiated thymidine per well, and incubated for further 12 hours when they were harvested, and incorporated radioactivity was then quantified.
Concentrations 0~20μM
Incubation time 4 days
Animal Experiment
Animal models DTH in mice
Formulation 10% DMSO
Dosages 50 mg/kg for 21 consecutive days
Administration intraperitoneal injections
Chemical Information
Molecular Weight 589.7
Formula C29H31N7O.CH4SO3
CAS Number 220127-57-1
Solubility (25°C) DMSO 60 mg/mL
Water 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Dietz AB, et al. Blood. Imatinib mesylate inhibits T-cell proliferation in vitro and delayed-type hypersensitivity in vivo.

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Keywords: Imatinib Mesylate, Gleevec, Glivec, CGP-57148B, STI-571 supplier, Src-bcr-Abl, inhibitors, activators

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