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 34 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.

    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.

  • 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.

    (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.
(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
Hep G2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPVUY4xUUN3ME2zNUDPxE1? NF7s[nYzPTh4M{KzNi=>
DU145 NYGwcW54S2WubDDWbYFjcWyrdImgRZN{[Xl? M3;oflIx6oDLzszN NWrBcHNiPi15MjDo MVfk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? MkXtNlU4QDZ4NU[=
PC3  NY\CNnR2S2WubDDWbYFjcWyrdImgRZN{[Xl? MkjiNlDjiIoQvF2= MVW2MVczKGh? MUnpcoNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? M1\FRVI2Pzh4NkW2
DU145 NFzZPXRCeG:ydH;zbZMhSXO|YYm= MYOyNQKBkc7:TR?= NFnvPVE1QC95MjDo MVHpcoR2[2W|IHPlcIwh\GWjdHigZpkh[XCxcITvd4l{ M3PjfVI2Pzh4NkW2
PC3  MX7BdI9xfG:|aYOgRZN{[Xl? MnryNlDjiIoQvF2= M{TqfFQ5Nzd{IHi= M2PHNYlv[3KnYYPld{Bk\WyuIIP1dpZqfmGu MUOyOVc5PjZ3Nh?=
MCF-7 NHrOZ4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vZNlExKM7:TR?= NGTOXVc1QCCq NWrV[|hW[myxY3vzJINmdGxicILvcIln\XKjdHnvckBqdmO{ZXHz[UBqdmS3Y3XkJIJ6KEKMM2q= MUKyOVI4PDB|NB?=
K-562  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPo[|k5UUN3ME2xJO69VQ>? NXvVfJdqOjV{M{m2OlI>
K562  MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\ETWM2OD1yLkZCpO69VQ>? MWOyOFk{QTRzOB?=
K562r MlX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTv[5poUUN3ME2xNOKh|ryP NVPrV442OjR7M{m0NVg>
K562 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrnVlFGSzVyPUCuNFkh|ryP MmnNNVY3Pzh2MUS=
K562 MUDDfZRwfG:6aXPpeJkhSXO|YYm= Ml;uNlQhcA>? MoXaTWM2OD1yLkKxJO69VQ>? Mn71NlIxODB{MEe=
MCF-7 MkDyR5l1d3SxeHnjbZR6KEG|c3H5 M1LGSlI1KGh? NWPoTlhJUUN3ME2wMlg{KM7:TR?= NGfmUnIzOjByMEKwOy=>
GIST882 MlnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jUPFk3KGh? MmW4TWM2OD1zLkeg{txO MnPzNlQ6ODB{MUK=

... 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]


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]
+ 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 Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
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


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 Conditions Sponsor/Collaborators Start Date Phases
NCT03674099 Recruiting Multiple Sclerosis Tomas Olsson|The Swedish Research Council|Karolinska Institutet October 1 2018 Phase 2
NCT03688568 Recruiting Neurofibroma Plexiform Indiana University|Food and Drug Administration (FDA) September 1 2018 Phase 2
NCT03516279 Not yet recruiting Chronic Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Minimal Residual Disease ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group August 12 2018 Phase 2
NCT02538926 Withdrawn 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) July 1 2018 Phase 2
NCT03131999 Recruiting Lymphangioleiomyomatosis Medical University of South Carolina|Columbia University January 23 2018 Phase 1|Phase 2
NCT03241199 Recruiting Chronic Myeloid Leukemia|Philadelphia Chromosome Positive CML The University of Hong Kong August 1 2017 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID