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    Imatinib Mesylate (STI571; Gleevec; Glivec)
    Imatinib Mesylate (STI571; Gleevec; Glivec)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0572
    CAS #: 220127-57-1Purity ≥98%

    Description: Imatinib Mesylate (also known as STI571 mesylate; trade names: Gleevec or Glivec), the mesylate salt of imatinib, is an orally bioavailable, potent, multi-kinase inhibitor of v-Abl, c-Kit and PDGFR with potential antitumor activity. It inhibits the aforementioned kinases with IC50 values of 0.6 μM, 0.1 μM and 0.1 μM in cell-free and/or cell-based assays, respectively. Imatinib acts by binding to the intracellular domain 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. Imatinib inhibits tyrosine kinases encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. 

    References: Proc Natl Acad Sci U S A. 1995 Mar 28; 92(7): 2558–2562; Int J Cancer. 2005 Feb 20;113(5):849-56.

    Related CAS #: 152459-95-5 (free base); 220127-57-1 (mesylate)   

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    Molecular Weight (MW)589.71
    FormulaC29H31N7O.CH4SO3
    CAS No.220127-57-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 118 mg/mL (200.1 mM)
    Water: <1 mg/mL
    Ethanol: 118 mg/mL (200.1 mM)
    Solubility (In vivo)Saline: 30 mg/mL
    SynonymsSTI571; CGP-57148B; ST-1571 Mesylate; CGP 57148; CGP57148; CGP-57148; CGP-57148B; CGP57148B; ; STI-571; STI 571; Imatinib mesylate; Brand name: Gleevec (USA); Glivec (other countries) 

    Chemical Name: N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide methanesulfonate

    SMILES Code: O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C)CC5)C=C4.CS(=O)(O)=O


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum to the murine PDGF receptor for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl2). After stimulation with PDGF (50 ng/mL) for 10 minutes at 4 °C, different concentrations of drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-33P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels.


    Cell Assay: BON-1 cells and NCI-H727 cells are seeded into flat-bottomed 96-well plates in triplicate and allowed to adhere overnight in 10% fetal bovine serum-supplemented DMEM or RPMI 1640 complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) or serum-free medium containing serial dilutions of Imatinib. After 48 hours (control cultures do not reach confluence), the number of metabolically active cells is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and absorbance is measured in a Packard Spectra microplate reader at 540 nm. Growth inhibition is calculated using the following formula: inhibition rate = (1 − a / b) × 100%, where a and b are the absorbance values of the treated and control groups, respectively.

    In VivoImatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation
    Animal model Female Swiss mice bearing SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers tumors.
    Formulation & Dosage Dissolved in water; 50, 70 mg/kg; i.p. injection
    References

    Proc Natl Acad Sci U S A. 1995 Mar 28; 92(7): 2558–2562; Int J Cancer. 2005 Feb 20;113(5):849-56.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Imatinib Mesylate

    Imatinib Mesylate

    Imatinib Mesylate

    Effect of compounds 1 (Imatinib), 2 (Sunitinib), and 35 on cKIT mediated signaling pathways in GIST-T1 and GIST-5R cancer cell lines.  2016 Sep 22;59(18):8456-72.


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