SU14813

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• Alarmwort

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SU14813 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  SU14813 (SU 014813) is a multi-receptor tyrosine kinase inhibitor with IC50 values of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit), respectively. It has potent antiangiogenic and antitumor activities.

• in vitro

  SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. It inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells) , PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR- 2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC ₅₀ values of 5.2, 9.9, and 11.2 nM, respectively. Also it inhibits the growth of U-118MG with an IC ₅₀ of 50 to 100 nM.

• in vivo

  SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduces growth of various established xenografts derived from human or rat tumor cell lines. Treatment in combination with docetaxel significantly enhances both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone.

• target

  < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> KIT
  (Cell-free assay)

  Target	Value
  VEGFR1 (Cell-free assay)	2 nM
  PDGFRβ (Cell-free assay)	4 nM
  15 nM
  VEGFR2 (Cell-free assay)	50 nM

SU14813 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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