Name: Imatinib Mesylate (STI571)
Price: 188.00 USD

- Overview
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    Background
    
    Imatinib mesylate is a tyrosine kinase inhibitor IC50 value of 100 nM, 100 nM, 600 nM for v-Abl, c-kit, PDGFR, respectively [1].Tyrosine kinase is an enzyme which is a subclass of protein kinase and plays an important role in transferring a phosphate group from ATP to a protein in cells. It is shown that tyrosine kinase plays a pivotal role in the management of disorders in which activation of c-Abl, PDGFR, or c-Kit signaling. Recently, the role of tyrosine kinases in the modulation of growth factor signaling are received more and more attention and gradually become an especial important target [2]. Imatinib Mesylate is a specific tyrosine kinase (abl, c-kit, and PDGFR) inhibitor and is reported to sensitize cells to radio- or chemo-therapy. When tested with Y-79 and WERI-RB-1 Rb cell lines, imatinib mesylate treatment decreased the cell proliferation and invasion with the concentration of 10 μM [3]. In osteoblast cells, administration of imatinib mesylate decreased osteoclast development via stimulating differentiation, inhibiting proliferation and survival [4].In dog model with mast cell tumor, administration of imatinib mesylate at a dose of 10 mg/kg daily for 1-9 weeks reduced tumor growth via inhibiting tyrosine kinase [5].
    
    [1].Buchdunger, E., et al., Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class. Proc Natl Acad Sci U S A, 1995. 92(7): p. 2558-62.
    [2].Zhou, Y., et al., The multi-targeted tyrosine kinase inhibitor vandetanib plays a bifunctional role in non-small cell lung cancer cells. Sci Rep, 2015. 5: p. 8629.
    [3].de Moura, L.R., et al., The effect of imatinib mesylate on the proliferation, invasive ability, and radiosensitivity of retinoblastoma cell lines. Eye (Lond), 2013. 27(1): p. 92-9.
    [4].O'Sullivan, S., et al., Imatinib mesylate does not increase bone volume in vivo. Calcif Tissue Int, 2011. 88(1): p. 16-22.
    [5].Isotani, M., et al., Effect of tyrosine kinase inhibition by imatinib mesylate on mast cell tumors in dogs. J Vet Intern Med, 2008. 22(4): p. 985-8.
- Properties
  - Alternative Name
    
    methanesulfonic acid;4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
    
    CAS Number
    
    220127-57-1
    
    Molecular Formula
    
    C29H31N7O·CH4SO3
    
    Molecular Weight
    
    589.71
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥29.5 mg/mL in DMSO; ≥2.84 mg/mL in EtOH with gentle warming and ultrasonic; ≥49.9 mg/mL in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Ivey MJ, Kuwabara JT, et al. "Platelet-derived growth factor receptor-α is essential for cardiac fibroblast survival." Am J Physiol Heart Circ Physiol. 2019 Aug 1;317(2):H330-H344. PMID:31125253

Imatinib Mesylate (STI571)

Imatinib Mesylate (STI571)

Background

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