Imatinib (STI571)

Imatinib 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.

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Imatinib (STI571) Chemical Structure

Imatinib (STI571) Chemical Structure
Molecular Weight: 493.6

Validation & Quality Control

Customer Reviews(4)

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description Imatinib 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.
Targets v-Abl PDGFR c-Kit
IC50 600 nM 100 nM [1] 100 nM [2]
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 μM, 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 μM, 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 μM, 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 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: [3]

Cell lines BON-1 cells and NCI-H727 cells
Concentrations ~100 μM
Incubation Time 48 hours
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) × 100%, where a and b are the absorbance values of the treated and control groups, respectively.

Animal Study: [5]

Animal Models SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).
Dosages 70 or 100 mg/kg
Administration Administered via i.p.
Solubility 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01650467 Not yet recruiting Leukemia, Myeloid, Chronic-Phase Centre Hospitalier Universitaire de Nmes 2013-10
NCT01781975 Not yet recruiting Diabetes Mellitus, Type I|Diabetes Mellitus, Insulin-Dependent, 1|Type 1 Diabetes Mellitus|Insulin-Dependent Diabetes Mellitus 1|IDDM University of California, San Francisco 2013-11 Phase 2
NCT01991379 Recruiting Gastrointestinal Stromal Tumor (GIST) Memorial Sloan-Kettering Cancer Center|Novartis 2013-11 Phase 1|Phase 2
NCT02013089 Recruiting Gastrointestinal Cancers Sun Yat-sen University 2013-12
NCT02001818 Not yet recruiting Chronic Myeloid Leukaemia Australasian Leukaemia and Lymphoma Group|Merck Sharp & Dohme (Australia) Pty Limited|Novartis Pharmaceuticals 2014-06 Phase 2

Chemical Information

Download Imatinib (STI571) SDF
Molecular Weight (MW) 493.6
Formula

C29H31N7O

CAS No. 152459-95-5
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms Glivec
Solubility (25°C) * In vitro DMSO 3 mg/mL (6 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name

Research Area

Customer Reviews (4)


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Rating
Source Leukemia Research 36 (2012) 1311– 1314. Imatinib (STI571) purchased from Selleck
Method Thymidine uptake Uptake assay
Cell Lines K562, MEG-01 cells
Concentrations 0.1-10 uM
Incubation Time 20 min
Results The effect of imatinib on nucleoside transport was first examined with thymidine. At a 10-M concentration, imatinib was able to inhibit the entry of radiolabeled thymidine in K562 cells by 76%. Imatinib was still efficient and blocked by 43% the entry of thymidine at 1 uM, but its effect on thymidine transport at 0.1 uM was not significant (Fig. 1a).

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Rating
Source Dr Helen Rizos from the university of Sydney. Imatinib (STI571) purchased from Selleck
Method Western blot
Cell Lines MelMS melanoma cell line
Concentrations 50 nM
Incubation Time 24/72 h
Results

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Rating
Source FASEB J 2011 25(10), 3661-3673. Imatinib (STI571) purchased from Selleck
Method Apoptosis assay
Cell Lines Ba/F3-p210T315I cells
Concentrations 0-5 μM
Incubation Time 24 h
Results In a parallel study using imatinib/PDMP or nilotinib/PDMP combinations, to our surprise, similar significant synergy in Ba/F3-p210T315I cells was observed.

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Rating
Source Dr Thomas Kruwel of Fraunhofer. Imatinib (STI571) purchased from Selleck
Method Cell Viability assay
Cell Lines A2C12/BetaD5/GammaA3/GammaD12/A549/CaCo2/HepG2 cell lines
Concentrations 0.0001-1000 nM
Incubation Time 24/96 h
Results

Product Citations (10)

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