Imatinib Mesylate (STI571)

Catalog No.S1026 Synonyms: CGP-57148B, ST-1571 Mesylate

Imatinib Mesylate (STI571) Chemical Structure

Molecular Weight(MW): 589.71

Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which 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 in cell-free or cell-based assays, respectively.

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In DMSO USD 191 In stock
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Cited by 55 Publications

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Biological Activity

Description Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which 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 in cell-free or cell-based assays, respectively.
Targets
PDGFR [1]
(Cell-free assay)		 c-Kit [2]
(M-07e cells)		 v-Abl [1]
(Cell-free assay)
100 nM 100 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 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T47D  M3nmZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{H3bmlEPTB;NUCg{txO M4fpcFI2QDZ|MkOy
Hep G2 NES5TodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnraTWM2OD1|MTFOwG0> NYrHWIRbOjV6NkOyN|I>
DU145 MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkK4NlDjiIoQvF2= MVW2MVczKGh? MkHL[IVkemWjc3XzJINmdGxidnnhZoltcXS7 NWLm[ZdOOjV5OE[2OVY>
PC3  M2DjdGNmdGxiVnnhZoltcXS7IFHzd4F6 M{W1PFIx6oDLzszN NELLT5A3NTd{IHi= NXTUfWZMcW6lcnXhd4V{KGOnbHygeoli[mmuaYT5 NImxb|IzPTd6Nk[1Oi=>
DU145 Mlz6RZBweHSxc3nzJGF{e2G7 MlftNlDjiIoQvF2= MlPCOFgwPzJiaB?= MV3pcoR2[2W|IHPlcIwh\GWjdHigZpkh[XCxcITvd4l{ NFr2XlUzPTd6Nk[1Oi=>
PC3  M3eyN2Fxd3C2b4Ppd{BCe3OjeR?= MYmyNQKBkc7:TR?= NHzCTWo1QC95MjDo NVPRdoVmcW6lcnXhd4V{KGOnbHygd5Vzfmm4YXy= MV:yOVc5PjZ3Nh?=
MCF-7 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj4SZB3OTBizszN Mm\ZOFghcA>? MV7icI9kc3NiY3XscEBxem:uaX\ldoF1cW:wIHnuZ5Jm[XOnIHnu[JVk\WRiYomgRmo{Yg>? Ml7DNlUzPzRyM{S=
K-562  MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTFizszN NVvXWpVZOjV{M{m2OlI>
K562  M3rMdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPqTWM2OD1yLkZCpO69VQ>? MVKyOFk{QTRzOB?=
K562r NU\5bnZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDQTWM2OD1zMNMg{txO M1XsO|I1QTN7NEG4
K562 MkfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXy1PVJtTUN3ME2wMlA6KM7:TR?= NIjTV3UyPjZ5OESxOC=>
K562 M4j2S2N6fG:2b4jpZ4l1gSCDc4PhfS=> NV7zXWp6OjRiaB?= M17tSWlEPTB;MD6yNUDPxE1? MorZNlIxODB{MEe=
MCF-7 MnGwR5l1d3SxeHnjbZR6KEG|c3H5 NX\UeIQzOjRiaB?= MlPQTWM2OD1yLkizJO69VQ>? Mn;rNlIxODB{MEe=
MDA-MB-23 M3jj[WN6fG:2b4jpZ4l1gSCDc4PhfS=> MVKyOEBp MlXkTWM2OD1zLkig{txO M{HDdFIzODByMkC3
GIST882 M4HRcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUW5OkBp NYT1fY9PUUN3ME2xMlch|ryP Mn\ENlQ6ODB{MUK=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-STAT5 / STAT5; 

PubMed: 18981115     


For phospho-STAT3 and Phospho-STAT5 detection, cells were then activated for 6 hrs with anti-CD3 and anti-CD28 Ab. Equivalent amounts of protein from cell lysates were separated by SDS-PAGE and western blot analysis was then performed using anti-phospho S䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖

p-ZAP70 / ZAP70 / p-LAT / LAT; 

PubMed: 18981115     


For the analysis of imatinib interference with early TCR signaling events, cells were activated for 5 min with anti-CD3 and anti-CD28 Abs and blots were probed with anti-phospho ZAP70, anti-ZAP70, anti-phospho LAT or anti-LAT antibodies. Untreated, non-ac䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 

18981115
Immunofluorescence
RelB; 

PubMed: 20371728     


Nuclear proteins were extracted from the untreated and treated cells and nuclear levels of RelA and RelB were confirmed by immunocytochemistry 

Cortactin / F-actin; 

PubMed: 20937825     


NIH3T3-SrcY527F cells were treated with DMSO or with 10 μm STI571 for 16 h, fixed and co-stained for cortactin (red, left panels) and F-actin (green, middle panels). Merged fields (right panels) demonstrate co-localization between cortactin and F-actin at䲧疝Ỵ疞㧀疜

20371728 20937825
Growth inhibition assay
Cell viability ; 

PubMed: 28435223     


(C) K562 cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. (D) KBM7R cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. 䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뾠Ղ䐺

28435223
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]

Protocol

Kinase Assay:[1]
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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 Research:[3]
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  • 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.
    (Only for Reference)
Animal Research:[5]
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  • Animal Models: SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).
  • Formulation: Imatinib is diluted in water.
  • Dosages: 70 or 100 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 118 mg/mL (200.09 mM)
Water 118 mg/mL (200.09 mM)
Ethanol 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 Information

Molecular Weight 589.71
Formula

C29H31N7O.CH4SO3
CAS No. 220127-57-1
Storage powder
in solvent
Synonyms CGP-57148B, ST-1571 Mesylate

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02687425 Unknown status Drug: Pioglitazone|Drug: imatinib mesylate Leukemia Myelogenous Chronic BCR-ABL Positive Meng Li|Tongji Hospital February 2016 Phase 2
NCT02303899 Unknown status Drug: Gemcitabine|Drug: Imatinib mesylate Mesothelioma Malignant Istituto Clinico Humanitas November 2014 Phase 2
NCT01898377 Active not recruiting Drug: Imatinib mesylate Mycophenolate mofetil Chronic Graft-versus-host Disease Seoul National University Hospital August 2013 Phase 2
NCT02891395 Completed Drug: Imatinib Mesylate and Nilotinib Graft Versus Host Disease University Hospital Lille|Novartis December 24 2012 Phase 2

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Bcr-Abl Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID