CP-547632 (hydrochloride)

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

CP-547632 (hydrochloride) Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  CP-547632 hydrochloride is an orally active, ATP-competitive VEGFR-2 and FGF kinase inhibitor with IC50 of 11 nM and 9 nM, respectively. It is selective for VEGFR2 and bFGF over EGFR, PDGFRβ and related tyrosine kinases (TKs), and has an antitumor effects.

• in vitro

  CP-547632 hydrochloride (1-1000 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC ₅₀ value of 6 nM.

  Western Blot Analysis

  Cell Line:	Serum-deprived cells
  Concentration:	1, 4, 16, 63, 250, 1000 nM
  Incubation Time:	1 hours
  Result:	Inhibited VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion.

• in vivo

  CP-547632 hydrochloride (po; 6.25-100 mg/kg/day; for 10-24 days) causes a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB- 231 xenografts.
  CP-547632 hydrochloride (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours.
  

  Animal Model:	Mice bearing tumors (75-150 mm in size)
  Dosage:	6.25, 12.5, 25, 50, 100 mg/kg
  Administration:	Po; daily; 10-24 days
  Result:	Caused a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts.

  < td class="col2"> H-ras tumor-bearing mice

  Animal Model:
  Dosage:	50 mg /kg
  Administration:	Oral
  Result:	A single oral dose of 50 mg/kg yielded plasma concentrations above 500 ng/ml for 12 hours.

• target

  VEGFR-2 < span> 11 nM (IC 50 )

  FGFR 9 nM (IC 50 )

CP-547632 (hydrochloride) Upstream-Materialien And Downstream Produkte

CP-547632 (hydrochloride) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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