1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. c-Kit
    Bcr-Abl
    PDGFR
    Autophagy

Imatinib Mesylate (Synonyms: CGP-57148B; STI-571)

Cat. No.: HY-50946 Purity: 99.90%
Data Sheet SDS Handling Instructions

Imatinib Mesylate is a known inhibitor of the c-Kit, Bcr-Abl, and PDGFR tyrosine kinases, inhibits the SLF-dependent activation of c-Kitwt kinase with IC50 of ~100 nM, which is similar to the concentration requires for inhibition of Bcr-Abl and PDGFR.

For research use only. We do not sell to patients.
Imatinib Mesylate Chemical Structure

Imatinib Mesylate Chemical Structure

CAS No. : 220127-57-1

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Customer Review

Other Forms of Imatinib Mesylate:

    Imatinib Mesylate purchased from MCE. Usage Cited in: J Bioenerg Biomembr. 2012 Feb;44(1):155-61.

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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Imatinib Mesylate is a known inhibitor of the c-Kit, Bcr-Abl, and PDGFR tyrosine kinases, inhibits the SLF-dependent activation of c-Kitwt kinase with IC50 of ~100 nM, which is similar to the concentration requires for inhibition of Bcr-Abl and PDGFR.

    IC50 & Target

    IC50: ~100 nM (c-Kit, Bcr-Abl, and PDGFR)[1]

    In Vitro

    Imatinib (STI571) Mesylate 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) mesylate 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) mesylate 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[3]. Imatinib mesylate selectively inhibits the activity of Bcr/Abl, c-Kit and PDGFR kinases. Imatinib mesylate reveals distinct and rapid antileukemic activity in chronic myelogenous leukemia (CML) and Philadelphia-positive (Ph+) acute lymphoblastic leukemia (ALL)[4].

    In Vivo

    Animals treated with Imatinib Mesylate show a decrease of mean body weight throughout the whole study. Body weight loss is noticeable in mice from groups that receive chemotherapy and the vitamin D analog combined treatment. The body weight decrease of mice treat with both combined Imatinib mesylate and PRI-2191 is the highest (15%) on Day 22 of the experiment, but after that day, mice start to recover[4]. In a rat Ischemia/reperfusion injury (IRI) model, Imatinib mesylate attenuates lung injury by an antipermeability and antiinflammatory effect. The delivery and function of Imatinib mesylate in the lung is also confirmed in this model[5].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.6957 mL 8.4787 mL 16.9575 mL
    5 mM 0.3391 mL 1.6957 mL 3.3915 mL
    10 mM 0.1696 mL 0.8479 mL 1.6957 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [4]

    Imatinib Mesylate is dissolved in DMSO and stored, and then diluted with appropriate media before use[4].

    Tested A549 cells are placed in 96-well flat-bottom plates at a density of 5×103 cells per well 24 h before the addition of the test compounds. The cells are incubated for 96 h with two different concentrations (10 and 100 nM) of PRI-2191 and concurrently with various concentrations of Imatinib mesylate (10, 100, 1000 and 10,000 ng/mL) and other cytostatic drugs (Docetaxel (DTX) or Idarubicin (ID) : 0.1, 1, 10, 100 ng/mL; Cisplatin (CIS): 1, 10, 100, 1000 ng/mL). The sulforhodamine B (SRB) assay is performed to evaluate the cytotoxic effect. As a result, IC50 is calculated for each separate experiment in Cheburator 0.4, Dmitry Nevozhay software[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4][5]

    Imatinib Mesylate is dissolved in DMSO and diluted in water (Mice)[4].
    Imatinib Mesylate (50 mg/kg) is dissolved in 0.5 mL of 20% DMSO (Rat)[5].

    Mice[4]
    NOD/SCID female mice, 12-16 weeks old, body weight of 20-25 g, are used. Mice are subcutaneously (s.c.) inoculated in the right flank of the abdomen with A549 tumor cells suspension (5×106 cells in 0.2 mL of Hank’s medium per mouse, Day 0) and then are randomized into groups receiving varied combinations of vitamin D analogs and chemotherapeutics. One out of two experimental protocols is applied in the respective experiments: 1. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 75 mg/kg/day, daily for 19 days (from Days 7-25). PRI-2191 is administered s.c. or by oral gavage at a dose of 2 μg/kg/day, 3 times a week (on Days 7, 12, 14, 16, 19, 21 and 23). 2. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 50 mg/kg/day, daily for 13 days (from Days 7-19). PRI-2191 and PRI-2205 are administered s.c. at doses of 1 or 10 μg/kg/day, respectively, 3 times a week (on Days 7, 10, 12, 14, 17, 19, 21, 24 and 26). At the end of the experiments, blood is collected under anesthesia; then, the mice are sacrificed.
    Rat[5]
    Male Lewis rats weighing 270 to 320 g are used in the experiments. Imatinib mesylate (50 mg/kg) is injected intraperitoneally in the Imatinib group (n=7), and 0.5 mL of 20% DMSO without Imatinib is administered in the vehicle group (n=7). The dose of 25 mg/kg is preliminarily tested, and it produces a little improvement in lung function without statistical significance. The dose of 50 mg/kg and intraperitoneal administration are adopted based on this result and past reports. The animals undergo left thoracotomy, and the left hilum is occluded with a small metallic clamp. The occlusion is performed 20 minutes after Imatinib or vehicle administration. During clamping, the tidal volume (TV) and respiratory rate (RR) are adjusted to 8 mL/kg and 80 breaths/min, respectively. After 90 minutes of ischemia, the clamp is removed and reperfusion is maintained for 120 minutes. During reperfusion, blood flow and ventilation are restored in the bilateral lung. In the sham group (n=6), the animals are heparinized, thoracotomized, and ventilated for 210 minutes. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.90%

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