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 29 Publications

5 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.

    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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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  MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVm3VowxUUN3ME21NEDPxE1? MlHLNlU5PjN{M{K=
Hep G2 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\B[FFKSzVyPUOxJO69VQ>? M{XiTVI2QDZ|MkOy
DU145 NUHU[2ZFS2WubDDWbYFjcWyrdImgRZN{[Xl? M3TXdFIx6oDLzszN MmHVOk04OiCq Mnvp[IVkemWjc3XzJINmdGxidnnhZoltcXS7 Ml7SNlU4QDZ4NU[=
PC3  MljER4VtdCCYaXHibYxqfHliQYPzZZk> M2TJOlIx6oDLzszN Mn;NOk04OiCq M{HlfYlv[3KnYYPld{Bk\WyuII\pZYJqdGm2eR?= NV;lUI5IOjV5OE[2OVY>
DU145 M1HqZ2Fxd3C2b4Ppd{BCe3OjeR?= MkDmNlDjiIoQvF2= M1Xjd|Q5Nzd{IHi= M1jVZYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCjcH;weI9{cXN? NVXxWG83OjV5OE[2OVY>
PC3  NX[zTmVTSXCxcITvd4l{KEG|c3H5 NEnnfXQzOOLCid88US=> NGfiNVA1QC95MjDo M2nkUYlv[3KnYYPld{Bk\WyuIIP1dpZqfmGu MYCyOVc5PjZ3Nh?=
MCF-7 NX3CcpA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HRd|ExKM7:TR?= NV3uNZl{PDhiaB?= NYHSUJAx[myxY3vzJINmdGxicILvcIln\XKjdHnvckBqdmO{ZXHz[UBqdmS3Y3XkJIJ6KEKMM2q= M{nKdVI2Ojd2MEO0
K-562  NIG0[VhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ixT2lEPTB;MTFOwG0> NH\FcYMzPTJ|OU[2Ni=>
K562  MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jXTGlEPTB;MD61xsDPxE1? MUKyOFk{QTRzOB?=
K562r MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\6UGlEPTB;MUFCpO69VQ>? MUWyOFk{QTRzOB?=
K562 NVzj[5A6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLFR|UxRTBwMEmg{txO Mny1NVY3Pzh2MUS=
K562 M{G3PGN6fG:2b4jpZ4l1gSCDc4PhfS=> NYi1XnNvOjRiaB?= NYfwWGp3UUN3ME2wMlIyKM7:TR?= M1\5NVIzODByMkC3
MCF-7 MXfDfZRwfG:6aXPpeJkhSXO|YYm= NXTqSYM3OjRiaB?= M2r6T2lEPTB;MD64N{DPxE1? M3nYfVIzODByMkC3
MDA-MB-23 MmT6R5l1d3SxeHnjbZR6KEG|c3H5 M3;YRlI1KGh? M3HlemlEPTB;MT64JO69VQ>? MV6yNlAxODJyNx?=
GIST882 NUjM[41jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LkUFk3KGh? MYrJR|UxRTFwNzFOwG0> MY[yOFkxODJzMh?=

... 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
+ 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
+ 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
+ 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 <1 mg/mL
In vivo Saline 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 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02709083 Not yet recruiting Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia Emory University December 2016 Phase 2
NCT02812693 Not yet 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 September 2016 Phase 1|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) August 2016 Phase 2
NCT02687425 Not yet recruiting Leukemia, Myelogenous, Chronic, BCR-ABL Positive Meng Li|Tongji Hospital February 2016 Phase 2
NCT02712112 Recruiting Gastrointestinal Stromal Tumors (GISTs) Asan Medical Center January 2016 Phase 2
NCT02644525 Not yet recruiting Loaisis National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) December 2015 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID