Search Site
Home >> Signaling Pathways >> TGF-β / Smad Signaling >> Bcr-Abl >> Imatinib Mesylate (STI571)
Related Biochemicals Related Antibodies

Imatinib Mesylate (STI571)

Multi-target kinase inhibitor of abl, c-kit, and PDGFR

Imatinib Mesylate (STI571)

Catalog No. A1805
Size Price Stock Qty
Evaluation Sample $28.00 In stock
100mg $100.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Imatinib Mesylate (STI571)

Related Biological Data

Imatinib Mesylate (STI571)

Related Biological Data

Imatinib Mesylate (STI571)

Biological Activity

Description Imatinib Mesylate (STI571), an orally bioavailability mesylate salt of Imatinib, 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, respectively.
Targets v-Abl PDGFR c-Kit      
IC50 600 nM 100 nM 100 nM      

Protocol

Cell experiment: [1]

Cell lines

T cells

Preparation method

Imatinib mesylate was dissolved in DMSO to a final concentration of 10 mM. The stock solution was stored at - 20°C until use, diluted to the final concentration in X-VIVO 15 medium, and added to cells immediately.

Reacting condition

IC50: 3.9 μM for inhibiting DCs-stimulated T-cell proliferation 2.9 μM for inhibiting PHA-stimulated T-cell proliferation 4 days

Applications

Cells were stimulated with allogeneic mature DCs or PHA in the presence of imatinib mesylate. The drug inhibited T-cell proliferation as a function of concentration. The effects were significant at 0.5 μM imatinib mesylate for the cells stimulated by DCs and at 1.0 μM imatinib mesylate for the cells stimulated with PHA. The IC50 values for imatinib mesylate–inhibited T-cell proliferation stimulated by DCs and PHA were 3.9 μM and 2.9 μM, respectively.

Animal experiment: [2]

Animal models

Female C57BL/6 mice

Dosage form

Intraperitoneal injection, 25 or 50mg/kg/day

Application

Administration of imatinib alone did not generate any changes in lung morphology. However, when imatinib was administered in bleomycin-treated mice, a reduction of fibrotic lesions in the subpleural areas of lung was observed at doses of 25 and 50 mg/kg/day. The quantitative histologic analysis demonstrated that the fibrotic score in mice treated with bleomycin and 50 mg/kg/day of imatinib was significantly lower than that treated with bleomycin alone. The collagen content of the lung was also significantly lower in mice treated with bleomycin and imatinib (50 mg/kg/day) as compared with those treated with bleomycin alone.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Dietz A B, Souan L, Knutson G J, et al. Imatinib mesylate inhibits T-cell proliferation in vitro and delayed-type hypersensitivity in vivo. Blood, 2004, 104(4): 1094-1099.

[2] Aono Y, Nishioka Y, Inayama M, et al. Imatinib as a novel antifibrotic agent in bleomycin-induced pulmonary fibrosis in mice. American journal of respiratory and critical care medicine, 2005, 171(11): 1279-1285.

Imatinib Mesylate (STI571) Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Imatinib Mesylate (STI571) Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 220127-57-1 SDF Download SDF
Chemical Name methanesulfonic acid;4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
Canonical SMILES CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5.CS(=O)(=O)O
Formula C29H31N7O.CH4SO3 M.Wt 589.71
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Research Update

2. Effects of imatinib mesylate on the spontaneous activity generated by the guinea-pig prostate. BJU Int. 2013 Aug;112(4):E398-405. doi: 10.1111/j.1464-410X.2012.11660.x.
Abstract
Although inconsistent results have been obtained from studies examining functional role of tyrosine kinase receptors in the generation of spontaneous activity in various segments of the gastrointestinal and urogenital tracts through imatinib mesylate, effects of imatinib mesylate on the spontaneous activity in the young and ageing prostate gland have been reported in detail.
4. Imatinib mesylate for plexiform neurofibromas in patients with neurofibromatosis type 1: a phase 2 trial. Lancet Oncol. 2012 Dec;13(12):1218-24. doi: 10.1016/S1470-2045(12)70414-X. Epub 2012 Oct 23.
Abstract
Imatinib mesylate has been evaluated for its efficacy to decrease the volume burden of plexiforn neurofibromas in NF1 patients.
5. Ageing is a risk factor in imatinib mesylate cardiotoxicity. Eur J Heart Fail. 2014 Feb 6. doi: 10.1002/ejhf.58. [Epub ahead of print]
Abstract
Imatinib mesylate, a tyrosine kinase inhibitor with anticancer activity, causes cardiotoxicity in patients.

Background

Imatinib mesylate is a small molecule that inhibits the c-Abl protein-tyrosine kinase, a kinase specifically important for proliferation of chronic myelogenous leukemia (CML). A translocation event between chromosomes 9 and 22 generates the Philadelphia c