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.

Size Price Stock Quantity  
In DMSO USD 191 In stock
USD 97 In stock
USD 197 In stock
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Cited by 31 Publications

6 Customer Reviews

  • THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m.

    Leukemia 2013 27, 932-40. Imatinib Mesylate (STI571) purchased from Selleck.

    Ba/F3-p210T315I cells were treated with indicated concentrations of imatinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P <0.05.

    FASEB J 2011 25, 3661-3673. Imatinib Mesylate (STI571) purchased from Selleck.

  • Inhibition of ER stress response protects against CBD-induced cell death. (b) LX-2 cells were treated with 5 μM CBD in serum-free media for 8 h in the presence or absence of 10 μM imatinib to inhibit ER stress. Expression of PARP, CHOP, and phospho-JNK was determined by western blot analysis and is presented as fold over vehicle.E.M. for n = four independent experiments. (c) Acid phosphatase activity was used to measure LX-2 cell viability following treatment with CBD and imatinib as in (b).

    Cell death dis 2011 2, e170. Imatinib Mesylate (STI571) purchased from Selleck.

    (a) Cell viability was measured by MTT assay after drug treatment. Results are shown as mean ± SD of at least three independent experiments. (b) Indicated cells were exposed to 0.3 μM imatinib for 3 h or 10 μM Y‐632 for 12 h and analyzed by Western blot.

    Cancer Sci, 2016, 107(6):782-90. Imatinib Mesylate (STI571) purchased from Selleck.

  • Cell Viability assay results. A2C12, BetaD5, GammaA3, GammaD12, A549, CaCo2, HepG2 cell lines were treated with imatinib mesylate for 24h and 96h.

     

     

    Dr. Thomas Kruwel of Fraunhofer-Institute for Toxicology and Experimental Medicine. Imatinib Mesylate (STI571) purchased 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.

    Dr. Helen Rizos from the university of Sydney. Imatinib Mesylate (STI571) purchased from Selleck.

Purity & Quality Control

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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  M{Xi[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVS5dWl7UUN3ME21NEDPxE1? NHfS[WQzPTh4M{KzNi=>
Hep G2 Ml\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTNzIN88US=> NIPZdlgzPTh4M{KzNi=>
DU145 NWDreG5ES2WubDDWbYFjcWyrdImgRZN{[Xl? NFTSWXMzOOLCid88US=> NIPoVYk3NTd{IHi= NEm4bYJl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= NGXWcVIzPTd6Nk[1Oi=>
PC3  NVW1c2VlS2WubDDWbYFjcWyrdImgRZN{[Xl? MoTWNlDjiIoQvF2= MofaOk04OiCq MX3pcoNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? M3fLe|I2Pzh4NkW2
DU145 M4T0TWFxd3C2b4Ppd{BCe3OjeR?= NEPQN5MzOOLCid88US=> M1LRPFQ5Nzd{IHi= M{fIRYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCjcH;weI9{cXN? MkHaNlU4QDZ4NU[=
PC3  NF\RSFNCeG:ydH;zbZMhSXO|YYm= MYSyNQKBkc7:TR?= MW[0PE84OiCq MWXpcoNz\WG|ZYOgZ4VtdCC|dYL2bZZidA>? MYSyOVc5PjZ3Nh?=
MCF-7 NV;TfXNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnq3NVAh|ryP NH\MN5U1QCCq NGjsblNjdG:la4OgZ4VtdCCycn;sbYZmemG2aX;uJIlv[3KnYYPlJIlv\HWlZXSgZpkhSkp|Wh?= NVX0TI17OjV{N{SwN|Q>
K-562  MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPMVpJKSzVyPUGg{txO NWHLbYZjOjV{M{m2OlI>
K562  NGHuTpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDvV5lTUUN3ME2wMlXDqM7:TR?= MVyyOFk{QTRzOB?=
K562r M4L0S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnsTWM2OD1zMNMg{txO MlSxNlQ6Ozl2MUi=
K562 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXFR|UxRTBwMEmg{txO NF3oRZkyPjZ5OESxOC=>
K562 NGLnXmREgXSxdH;4bYNqfHliQYPzZZk> M3XGfVI1KGh? M2PCSWlEPTB;MD6yNUDPxE1? NHjyVGYzOjByMEKwOy=>
MCF-7 MluwR5l1d3SxeHnjbZR6KEG|c3H5 MX6yOEBp NHKxVZpKSzVyPUCuPFMh|ryP M{\pdlIzODByMkC3
MDA-MB-23 MnHjR5l1d3SxeHnjbZR6KEG|c3H5 M4HGc|I1KGh? M3fZT2lEPTB;MT64JO69VQ>? M1LVNFIzODByMkC3
GIST882 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DSd|k3KGh? NXraWmdOUUN3ME2xMlch|ryP MYOyOFkxODJzMh?=

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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 slightly soluble or insoluble
In vivo Add solvents individually and in order:
Saline
30 mg/mL

* 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
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Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00044304 Recruiting Hypereosinophilic Syndrome National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) August 22, 2002 Phase 2
NCT02644525 Not yet recruiting Loaisis National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) December 21, 2015 Phase 2
NCT03007147 Not yet recruiting B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|BCR-ABL1 Fusion Protein Expression|Minimal Residual Disease|Philadelphia Chromosome Positive|T Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia Childrens Oncology Group|National Cancer Institute (NCI) July 2017 Phase 3
NCT03023046 Not yet recruiting Adult Acute Lymphoblastic Leukemia|Adult Lymphoblastic Lymphoma|CD20 Positive|Philadelphia Chromosome Positive University of Washington|National Cancer Institute (NCI) February 2017 Phase 2
NCT02538926 Not yet recruiting B Acute Lymphoblastic Leukemia|B Lymphoblastic Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent B Lymphoblastic Lymphoma|Recurrent T Lymphoblastic Leukemia/Lymphoma|Refractory B Lymphoblastic Lymphoma|Refractory T Lymphoblastic Lymphoma|T Acute Lymphoblastic Leukemia|T Lymphoblastic Lymphoma University of Washington|National Cancer Institute (NCI) January 2017 Phase 2
NCT02812693 Recruiting Stage IIIA Skin Melanoma|Stage IIIB Skin Melanoma|Stage IIIC Skin Melanoma|Stage IV Skin Melanoma Joanne Jeter|National Cancer Institute (NCI)|Merck Ltd.|Ohio State University Comprehensive Cancer Center November 2016 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID