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Imatinib Mesylate

Imatinib Mesylate

Item no.	S1026-5000
Manufacturer	Selleckchem
CASRN	220127-57-1
Amount	5 g
Category	Oncology Neuroscience Metabolism Glucose Homeostasis Cholesterol & Lipid Metabolism Aging & Neurological Disorders Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Skin Cancer Colorectal Cancer Heart & Blood Cancer
Type	Inhibitors
Specific against	other
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	Gleevec, Glivec, CGP-57148B
Similar products	Imatinib
Available
Administration	Administered via i.p.
Animal Models	SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).
Cell lines	BON-1 cells and NCI-H727 cells
Chemical Name	N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide methanesulfonic acid
Clinical Trials	Imatinib is currently being investigated in Phase III clinical trials in patients with Sarcoma.
Concentrations	ca.100 uM
Description	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 uM, 0.1 uM and 0.1 uM, respectively.
Dosages	70 or 100 mg/kg
Formulation	Imatinib is diluted in water.
IC50	600 nM, 600 nM, 600 nM, 600 nM, 600 nM, 600 nM
In vitro	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 uM, respectively. [1] Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 uM, which is similar to the concentration required for inhibition of PDGFR. [2] 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 uM, respectively. [3], 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. [4]
In vivo	Imatinib 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. [5], 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. [6]
Incubation Time	48 hours
Kinase Assay	PDGF receptor kinase activity, 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 uCi [7-33P]-ATP and l uM ATP for 10 minutes at 4 C. Immune complexes are separated by SDS-PAGE on 7.5% gels.
Method	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) x 100%, where a and b are the absorbance values of the treated and control groups, respectively.
Molecular Weight (MW)	589, 71
Picture ChemicalStructure Description	Imatinib Mesylate Chemical Structure
Picture Description 1	, , Dr. Helen Rizos from the university of Sydney, Imatinib Mesylatepurchased from Selleck, A. Viability curve for the c-Kit mutant MelMS melanoma cell line treated with increasing concentrations of imatinib for 72h (relative to DMSO-treated controls, mean sd, n=3) B. MelMS melanoma cells were treated with 50nM imatinib for 24h. The effects on c-Kit, ERK and AKT activation were determined by immunoblotting.
Picture Description 2	, , Dr Thomas Kruwel of Fraunhofer-Institute for Toxicology and Experimental Medicine, Imatinib Mesylatepurchased from Selleck, Cell Viability assay results. A2C12, BetaD5, GammaA3, GammaD12, A549, CaCo2, HepG2 cell lines were treated with imatinib mesylate for 24h and 96h.
Solubility (25C)	DMSO 118 mg/mL, Water 118 mg/mL, Ethanol <1 mg/mL
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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