2. Protein Tyrosine Kinase/RTK Anti-infection Autophagy
  3. Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy
  4. Imatinib

Imatinib  (Synonyms: STI571; CGP-57148B)

Cat. No.: HY-15463 Purity: 99.95%
COA Handling Instructions

Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.

For research use only. We do not sell to patients.

Imatinib Chemical Structure

Imatinib Chemical Structure

CAS No. : 152459-95-5

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Customer Review

Based on 73 publication(s) in Google Scholar

Other Forms of Imatinib:

Imatinib Related Antibodies

Top Publications Citing Use of Products

66 Publications Citing Use of MCE Imatinib

WB
Proliferation Assay
IHC

    Imatinib purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4.  [Abstract]

    Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in PC-9 GR NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.

    Imatinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Apr 24;9(31):22158-22183.  [Abstract]

    Primary tumors are dissected at the end of experiment and subjected to immunohistochemistry. Representative images of primary tumor sections stained with anti-PCNA (proliferation), anti-cleaved caspase 3 (apoptosis), and anti-CD31 (angiogenesis).

    Imatinib purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Jun 1;12(6):e0178619.  [Abstract]

    The protein expression of PDGF-A, PDGF-B, PDGF-C, and PDGF-D in hearts from mice treated with vehicle, Imatinib (IMA), ISO, IMA+ISO for one week is tested by Western blot.

    Imatinib purchased from MedChemExpress. Usage Cited in: Med Sci Monit. 2017 Aug 6;23:3808-3816.  [Abstract]

    The kinase activity of c-Kit is enhanced in an animal model of cardiac fibrosis. The lysates of heart tissues from a mice model treated with vehicle, Imatinib (IMA), ISO, or Imatinib + ISO for one week are analyzed for phosphorylation level of p-c-Kit (Tyr719) and total protein level of c-Kit. The western blotting results from one mouse in each group and the statistical analysis of the western blotting bands are shown.

    Imatinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 15;8(67):111110-111118.  [Abstract]

    In cell EC50 determination of CHMFL-KIT-031 with parental Colo320DM (KIT wt) and KIT V559D overexpressed Colo320DM cells.

    Imatinib purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Sep 22;59(18):8456-72.  [Abstract]

    Effect of compounds 1 (Imatinib), 2 (Sunitinib), and 35 on cKIT mediated signaling pathways in GIST-T1 and GIST-5R cancer cell lines.

    Imatinib purchased from MedChemExpress. Usage Cited in: J Bioenerg Biomembr. 2012 Feb;44(1):155-61.  [Abstract]

    Differences in sensitivity of PDR-mutants to 3-BP, Imatinib methanesulfonate, Daunorubicin and Rhodamine 6 G. Minimal medium (YNB) with sucrose.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively[1][2][3][4]. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV[5].

    IC50 & Target

    BCR/ABL, v-Abl, PDGFR, c-kit[1][2][4]
    In Vitro

    Imatinib (STI571) inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering total protein levels of c-kit, MAPK, or Akt. The concentration that produces 50% inhibition for these effects is approximately 100 nM[1].
    Imatinib (STI571) is very effective (in vitro IC50 of 25 nM) against the chronic myeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (in vitro IC50, 410 nM) and PDGFR (in vitro IC50, 380 nM)[2].
    Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and inhibits Bcr/Abl, v-Abl, Tel/Abl, the native PDGFβ receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylation and cell growth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFβR, and Tel/Arg with an IC50 of approximately 0.5 μM in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2[4].
    The IC50s of Imatinib(STI571) is a multi-target inhibitor of v-Abl, c-Kit and on BON-1 and H727 cells after exposure for 48 h are 32.4 and 32.8 μM, respectively[6].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Imatinib Related Antibodies
    In Vivo

    In the phosphorothioate antisense oligodeoxynucleotides (PS-ASODN) group, tumor growth is inhibited by 59.437%, which is markedly higher than in the Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and group (11.071%) and liposome negative control group (2.759%). Telomerase activity is significantly lower (P<0.01) in the PS-ASODN group (0.689±0.158) compare with the Imatinib group (1.838±0.241), liposome negative control group (2.013±0.273), and saline group (2.004±0.163)[7].
    Imatinib (25 mg/kg/day, p.o.) suppresses the growth of endometriotic tissue and reduces the number of ovarian follicles in a rat model. Imatinib effectively treats experimental endometriosis by its inhibitor effects on angiogenesis and cell proliferation[8].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    493.60

    Appearance

    Solid

    Formula

    C29H31N7O
    CAS No.
    SMILES

    CN(CC1)CCN1CC2=CC=C(C(NC3=CC=C(C)C(NC4=NC(C5=CC=CN=C5)=CC=N4)=C3)=O)C=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 12.5 mg/mL (25.32 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0259 mL 10.1297 mL 20.2593 mL
    5 mM 0.4052 mL 2.0259 mL 4.0519 mL
    10 mM 0.2026 mL 1.0130 mL 2.0259 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 11 mg/mL (22.29 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.25 mg/mL (2.53 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.25 mg/mL (2.53 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 1.25 mg/mL (2.53 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.95%

    COA (265 KB) LCMS (265 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [4]

    BON-1 cells (7,500 per well) and NCI-H727 cells (5,000 per well) 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 h (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. Experiments are done in triplicates[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [6][7]

    Mice[6]
    The 40 tumor-bearing SCID mice are randomly divided into four groups (10 mice per group): the PS-ASODN group (5 μM, each mouse receives 0.2 mL by intratumor injection once daily); Imatinib group (0.1 mg/g body weight); liposome negative control group (0.01 mL/g); and saline group (0.01 mL/g). The mice in each group receive the relevant treatment by intra-tumor injection once daily from day 7 to day 28 after implantation. After 28 d, the mice are sacrificed, and tumor weight and longest and shortest diameters are measured by electronic scale and vernier caliper, respectively. Inhibition of tumor growth is calculated.
    Rats[7]
    Adult female Wistar-Albino rats (220-240 g) are used. Twenty-one days after the first surgical procedure, the rats undergo a second laparotomy to evaluate the occurrence of endometriosis. Twenty-four rats have visually confirmed endometriotic implants and are randomized into three groups to receive Imatinib (25 mg/kg/day, p.o.), Anastrozole (0.004 mg/day, p.o.), or normal saline (0.1 mL, i.p.) for 14 days.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Imatinib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Imatinib152459-95-5STI571 CGP-57148BSTI 571STI-571Bcr-AblPDGFRc-KitSARS-CoVAutophagyPlatelet-derived growth factor receptorSCFRCD117SARS coronavirusInhibitorinhibitorinhibit

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