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.

    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.
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{DYXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjSNFRKSzVyPUWwJO69VQ>? M3zsU|I2QDZ|MkOy
Hep G2 MnK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjS[IRKSzVyPUOxJO69VQ>? MVKyOVg3OzJ|Mh?=
DU145 MWLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3nKTVIx6oDLzszN M1uxXVYuPzJiaB?= MWnk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? MmrWNlU4QDZ4NU[=
PC3  M3zNbGNmdGxiVnnhZoltcXS7IFHzd4F6 MXyyNQKBkc7:TR?= M1H5bVYuPzJiaB?= MojSbY5kemWjc3XzJINmdGxidnnhZoltcXS7 NF3wW|kzPTd6Nk[1Oi=>
DU145 MYXBdI9xfG:|aYOgRZN{[Xl? NELRWHIzOOLCid88US=> MorzOFgwPzJiaB?= NU\FNIRDcW6mdXPld{Bk\WyuIHTlZZRpKGK7IHHwc5B1d3Orcx?= NE\SeoIzPTd6Nk[1Oi=>
PC3  NVvSdJhKSXCxcITvd4l{KEG|c3H5 MYmyNQKBkc7:TR?= NYTiNZI1PDhxN{KgbC=> NFX0THlqdmO{ZXHz[ZMh[2WubDDzeZJ3cX[jbB?= MY[yOVc5PjZ3Nh?=
MCF-7 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrKc|AyOCEQvF2= NYjNUnZOPDhiaB?= M4qxUIJtd2OtczDj[YxtKHC{b3zp[oVz[XSrb36gbY5kemWjc3WgbY5lfWOnZDDifUBDUjOc M3jNclI2Ojd2MEO0
K-562  NUXVO4FyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrtd3RKSzVyPUGg{txO M{LFc|I2OjN7Nk[y
K562  Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPrb5pKSzVyPUCuOeKh|ryP MoP1NlQ6Ozl2MUi=
K562r NHnFOGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFKxS5NKSzVyPUGwxsDPxE1? MlvwNlQ6Ozl2MUi=
K562 MnrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPUOHZGSzVyPUCuNFkh|ryP M1O4blE3Pjd6NEG0
K562 NHXjSplEgXSxdH;4bYNqfHliQYPzZZk> MkH4NlQhcA>? MnPsTWM2OD1yLkKxJO69VQ>? Mn3XNlIxODB{MEe=
MCF-7 NUL4TFlQS3m2b4TvfIlkcXS7IFHzd4F6 NGXnXZczPCCq M4PRWWlEPTB;MD64N{DPxE1? M2LHSFIzODByMkC3
MDA-MB-23 MorCR5l1d3SxeHnjbZR6KEG|c3H5 MXiyOEBp MVfJR|UxRTFwODFOwG0> MWeyNlAxODJyNx?=
GIST882 M1HGXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M36wVlk3KGh? NUP6d3V4UUN3ME2xMlch|ryP NVjU[oxUOjR7MECyNVI>

... 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 Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
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
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):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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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)
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Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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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Bcr-Abl Signaling Pathway Map

Bcr-Abl Inhibitors with Unique Features

  • Selective Bcr-Abl Inhibitor

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  • Most Potent Bcr-Abl Inhibitor

    GZD824 : Bcr-Abl(WT), IC50=0.34 nM; Bcr-Abl(T315I), IC50=0.68 nM.

  • FDA-approved Bcr-Abl Inhibitor

    Dasatinib : Approved by FDA for CML and Ph+ ALL.

  • Newest Bcr-Abl Inhibitor

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID