SU5614

SU5614

Catalog Number:
L002371428APE
Mfr. No.:
APE-B6097
Price:
$220
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          Background

          IC50: 100 nM for FLT3 inhibitionSU5614 is a protein tyrosine kinase inhibitor.Tyrosine kinases are enzymes for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein. In vitro: Previous study found that SU5614 could induce growth arrest and apoptosis in c-kit-expressing Kasumi-1, M-07e, and UT-7 cells and inhibited the stem cell factor (SCF)-induced tyrosine phosphorylation of c-kit. Moreover, the sensitivity of Kasumi-1 cells towards the growth inhibitory activity of SU5614 was mainly caused by an autocrine production of SCF, but not by the transforming mutations of c-kit [1]. In vivo: It was found that administration of SU5614, a vascular endothelial growth factor (VEGF) inhibitor, to mice could reduce the levels of VEGF dramatically in BAL fluids 72 h after toluene diisocyanate inhalation. Moreover, consistent with the results obtained from the enzyme immunoassays, Western blot analyses showed that SU5614 reduced the levels of VEGF in the BAL fluid 72 h after toluene diisocyanate inhalation. These results suggested that VEGF might be one of the major determinants of toluene diisocyanate -induced asthma and that the inhibition of VEGF might be a good therapeutic strategy [2]. Clinical trial: Up to now, SU5614 is still in the preclinical development stage.

          [1] Spiekermann K,Faber F,Voswinckel R,Hiddemann W. The protein tyrosine kinase inhibitor SU5614 inhibits VEGF-induced endothelial cell sprouting and induces growth arrest and apoptosis by inhibition of c-kit in AML cells. Exp Hematol.2002 Jul;30(7):767-73.
          [2] Lee YC,Kwak YG,Song CH. Contribution of vascular endothelial growth factor to airway hyperresponsiveness and inflammation in a murine model of toluene diisocyanate-induced asthma. J Immunol.2002 Apr 1;168(7):3595-600.

      • Properties
        • Alternative Name
          (Z)-5-chloro-3-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)indolin-2-one
          CAS Number
          1055412-47-9
          Molecular Formula
          C15H13ClN2O
          Molecular Weight
          272.73
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥27.3 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
          Storage
          Store at -20°C

          * For Research Use Only

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