ZD-4190

Catalog No.S6543

ZD-4190 Chemical Structure

Molecular Weight(MW): 459.27

ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.

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Biological Activity

Description ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
Targets
KDR [1]
()
Flt-1 [1]
()
In vitro

ZD4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with greatest effect against KDR. Selectivity versus FGFR1 tyrosine kinase activity is demonstrated, with at least a 30-fold difference in the IC50 required to inhibit HUVEC proliferation stimulated by VEGF or bFGF, respectively. No effects on basal HUVEC growth are observed, even at the maximum ZD4190 concentration examined in these assays (10 μM)[1].

In vivo

Chronic once-daily oral dosing of ZD4190 to young rats produces a dose-dependent increase in the femoral epiphyseal growth plate area. Once-daily oral dosing of ZD4190 to mice bearing established (∼0.5 cm3) human tumor xenografts (breast, lung, prostate, and ovarian) elicits significant antitumor activity and at doses that would not be expected to have any direct antiproliferative effect on tumor cells. In a PC-3 xenograft model, 10 weeks of ZD4190 dosing prolongs tumor cytostasis and upon withdrawal of therapy, tumor growth resumed after a short delay[1].

Protocol

Animal Research:

[1]

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  • Animal Models: Young female Alderley Park rats (Wistar derived, 150 g in weight, 4-8 weeks of age)
  • Formulation: 1% (v/v) solution of polyoxyethylene sorbitan mono-oleate in deionized water
  • Dosages: 15, 50, and 150 mg/kg/day
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

Chemical Information

Molecular Weight 459.27
Formula

C19H16BrFN6O2

CAS No. 413599-62-9
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID