Imatinib Mesylate (STI571; Gleevec; Glivec)

Alias: STI571; CGP-57148B; ST-1571 Mesylate; CGP 57148; CGP57148; CGP-57148; CGP-57148B; CGP57148B; ; STI-571; STI 571; Imatinib mesylate; Brand name: Gleevec (USA); Glivec (other countries)
Cat No.:V0572 Purity: =99.89%
Imatinib Mesylate (also known as STI571 mesylate; trade names: Gleevec or Glivec), the mesylate salt of imatinib, is an orally bioavailable,potent,multi-kinase inhibitor of v-Abl, c-Kit and PDGFR with potential antitumor activity.
Imatinib Mesylate (STI571; Gleevec; Glivec) Chemical Structure CAS No.: 220127-57-1
Product category: c-Kit
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: =99.89%

Purity: ≥98%

Product Description

Imatinib Mesylate (also known as STI571 mesylate; trade names: Gleevec or Glivec), the mesylate salt of imatinib, is an orally bioavailable, potent, multi-kinase inhibitor of v-Abl, c-Kit and PDGFR with potential antitumor activity. It inhibits the aforementioned kinases with IC50 values of 0.6 μM, 0.1 μM and 0.1 μM in cell-free and/or cell-based assays, respectively. Imatinib acts by binding to the intracellular domain located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. Imatinib inhibits tyrosine kinases encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes.

Biological Activity I Assay Protocols (From Reference)
c-Kit (IC50 ~100 nM); Bcr-Abl (IC50 ~100 nM); PDGFR (IC50 ~100 nM)
ln Vitro
Imatinib (STI571) Mesylate prevents c-Kit autophosphorylation, MAPK activation, and Akt activation without changing the overall amounts of c-kit, MAPK, or Akt protein. About 100 nM is the concentration that results in 50% inhibition for these effects[1]. The kinase Bcr-Abl that causes chronic myeloid leukemia is highly susceptible to imatinib (STI571) mesylate (in vitro IC50 of 25 nM). Moreover, imatinib effectively inhibits PDGFR (in vitro IC50, 380 nM) and Kit (in vitro IC50, 410 nM)[2]. Imatinib (STI571) mesylate is a multi-target inhibitor of v-Abl, c-Kit, and it also inhibits the native PDGFβ receptor, Bcr/Abl, v-Abl, Tel/Abl, and c-Kit. However, it does not inhibit the EGFR, c-Fms, Flt3, Src family kinases, or numerous other tyrosine kinases. Imatinib has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2[3]. However, it inhibits the 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. Imatinib mesylate specifically impedes c-Kit, PDGFR kinase, and Bcr/Abl activity. In patients with Philadelphia-positive (Ph+) acute lymphoblastic leukemia (ALL) and chronic myelogenous leukemia (CML), imatinib mesylate exhibits unique and swift antileukemic activity[4].
ln vivo
Imatinib has varying antitumor effects on three xenografted tumors made from surgical samples of newly diagnosed human small cell lung cancers: the growth of the SCLC6, SCLC61, and SCLC108 tumors is inhibited by 80%, 40%, and 78%, respectively, while the growth of SCLC74 is not significantly affected. When administered by gavage at 10, 20, and 40 mg/kg, respectively, Imatinib significantly reduces the high fat-induced lipid staining area in ApoE(-/-) mice fed a high fat diet by 30%, 27%, and 35% compared to high fat diet untreated controls and suppresses carotid artery lipid accumulation.
Enzyme Assay
Rabbit antiserum is used to immunoprecipitate the PDGF receptor from extracts of BALB/c 3T3 cells, which is then left on ice for two hours. Antigen-antibody complexes are gathered using protein A-Sepharose beads. TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and kinase buffer (20 mM Tris, pH 7.5, 10 mM MgCl2) are the three solutions used to wash the immunoprecipitates twice. A variety of drug concentrations are added to the reaction mixture after PDGF (50 ng/mL) stimulation for 10 minutes at 4°C.
Cell Assay
Twenty-four hours before the test compounds are added, tested A549 cells are arranged at a density of 5×103 cells per well in 96-well flat-bottom plates. In addition to different doses of Imatinib mesylate (10, 100, 1000, and 10,000 ng/mL) and other cytostatic medications (Docetaxel (DTX) or Idarubicin (ID): 0.1, 1, 10, 100 ng/mL; Cisplatin (CIS): 1, 10, 100, 1000 ng/mL), the cells are incubated with PRI-2191 at two different concentrations (10 and 100 nM) for 96 hours. The assay known as sulforhodamine B (SRB) is utilized to assess the cytotoxic effect. As a result, the Dmitry Nevozhay software Cheburator 0.4 calculates the IC50 for every individual experiment[4].
Animal Protocol
Mice: We use female NOD/SCID mice that are 12–16 weeks old and weigh 20–25 g. On Day 0, mice receive a subcutaneous (s.c.) inoculation of A549 tumor cells suspension (5×106 cells in 0.2 mL of Hank's medium per mouse). Following this, they are randomly assigned to groups that receive different combinations of vitamin D analogs and chemotherapeutics. In the corresponding experiments, one of the two experimental protocols is used: 1. After the tumor cells are injected, treatment begins on Day 7 (when the tumors become palpable). For 19 days (from Days 7 to 25), imatinib mesylate is given intraperitoneally (i.p.) at a dose of 75 mg/kg/day. PRI-2191 is given orally or s.c. three times a week (on Days 7, 12, 14, 16, 19, 21, and 23) at a dose of 2 μg/kg/day. 2. After tumor cells are injected, treatment begins on Day 7 (when tumors become palpable). For 13 days (from Days 7-19), imatinib mesylate is given intraperitoneally (i.p.) at a dose of 50 mg/kg/day. PRI-2191 and PRI-2205 are given subcutaneously (s.c.) three times a week (on Days 7, 10, 12, 14, 17, 19, 21, 24, and 26) at doses of 1 or 10 μg/kg/day, respectively. Blood is drawn while the mice are sedated at the conclusion of the trials, and they are then killed.
Rats: In the experiments, male Lewis rats weighing between 270 and 320 g are employed. The Imatinib group (n = 7) receives an intraperitoneal injection of Imatinib mesylate (50 mg/kg), while the vehicle group (n = 7) receives 0.5 mL of 20% DMSO without Imatinib. Preliminary testing reveals that the 25 mg/kg dose slightly improves lung function without reaching statistical significance. Based on previous reports and this result, the intraperitoneal administration of 50 mg/kg was chosen. The animals have a left thoracotomy, and a tiny metallic clamp is used to occlude the left hilum. The occlusion is carried out 20 minutes following the administration of imatinib or the vehicle. Tidal volume (TV) and respiratory rate (RR) are set to 8 mL/kg and 80 breaths/min, respectively, during clamping. The clamp is taken off after 90 minutes of ischemia, and reperfusion is sustained for an additional 120 minutes. The bilateral lung's blood flow and ventilation are restored during reperfusion. The animals in the sham group (n=6) undergo 210 minutes of ventilation, thoracotomy, and heparinization.

[1]. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32.

[2]. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9.

[3]. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8.

[4]. Vitamin D Analogs Potentiate the Antitumor Effect of Imatinib Mesylate in a Human A549 Lung Tumor Model. Int J Mol Sci. 2015 Nov 13;16(11):27191-207.

[5]. Protective Effects of Imatinib on Ischemia/Reperfusion Injury in Rat Lung. Ann Thorac Surg. 2016 Jul 23. pii: S0003-4975(16)30523-9.

[6]. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
Molecular Weight
Exact Mass
Elemental Analysis
C, 61.10; H, 5.98; N, 16.63; O, 10.85; S, 5.44
Related CAS #
152459-95-5; 220127-57-1 (mesylate)
white to off-white to brownish or yellowish tinged crystalline powder
InChi Key
InChi Code
Chemical Name
methanesulfonic acid;4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
STI571; CGP-57148B; ST-1571 Mesylate; CGP 57148; CGP57148; CGP-57148; CGP-57148B; CGP57148B; ; STI-571; STI 571; Imatinib mesylate; Brand name: Gleevec (USA); Glivec (other countries)
HS Tariff Code

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~118 mg/mL (~200.1 mM)
Water: <1 mg/mL
Ethanol: ~118 mg/mL (~200.1 mM)
Solubility (In Vivo)
Saline: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.


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Working concentration mg/mL;

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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01742299 Active
Drug: imatinib mesylate GIST and CML Novartis Pharmaceuticals March 26, 2013 Phase 4
NCT01738139 Active
Drug: Imatinib Mesylate
Biological: Ipilimumab
Metastatic Melanoma
Unresectable Melanoma
M.D. Anderson Cancer Center February 19, 2013 Phase 1
NCT04416750 Active
Drug: Imatinib Mesylate Pulmonary Arterial Hypertension Imperial College London January 20, 2021 Phase 2
NCT05623774 Recruiting Drug: Imatinib Mesylate
Drug: IkT-001Pro
CML Inhibikase Therapeutics, Inc. December 16, 2022 Phase 1
NCT05385549 Recruiting Drug: Imatinib Mesylate Gastrointestinal Stromal Tumors Asan Medical Center September 7, 2022 Phase 2
Biological Data
  • Imatinib Mesylate

  • Imatinib Mesylate
  • Imatinib Mesylate

    Effect of compounds 1 (Imatinib), 2 (Sunitinib), and 35 on cKIT mediated signaling pathways in GIST-T1 and GIST-5R cancer cell lines.2016 Sep 22;59(18):8456-72.

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