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Imatinib Mesylate

Cat. No. M1799
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 31.5  USD35 In stock
500mg USD 81  USD90 In stock
1g USD 135  USD150 In stock
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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
Cell Experiment
Cell lines T cells
Preparation method Cell proliferation assays. T cells, 1 × 105 in 200 μL/well of 96-well microtiter plates (Corning, Corning, NY), were stimulated with DCs or phytohemagglutinin M (PHA-M; 10 μg/mL, Sigma) or PDGF or both (R&D Systems, Minneapolis, MN) 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 (Amersham, Arlington Heights, IL) 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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 589.7
Formula C29H31N7O.CH4SO3
CAS Number 220127-57-1
Purity 99.86%
Solubility DMSO 60 mg/mL
Water 60 mg/mL
Storage at -20°C
References

Imatinib mesylate inhibits T-cell proliferation in vitro and delayed-type hypersensitivity in vivo.
Dietz AB, et al. Blood. 2004 Aug 15;104(4):1094-9. PMID: 15100154.

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

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