(E)-3-(3-bromo-4,5-dihydroxyphenyl)-N-(3,4,5-trihydroxybenzyl)prop-2-enethioamide

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

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

(E)-3-(3-bromo-4,5-dihydroxyphenyl)-N-(3,4,5-trihydroxybenzyl)prop-2-enethioamide Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  nt157 is an irs-1/2 inhibitor.insulin receptor substrates 1 and 2 (irs1/2) mediate antiapoptotic and mitogenic signaling from insulin receptor (ir), insulin-like growth factor 1 receptor (igf-ir), and other oncoproteins. irs1 plays a critical role in cancer cell proliferation, and its expression is increased in many human malignancies.

• in vitro

  nt157 treatment was fonund to be able to lead to dose-dependent suppression of irs protein expression, inhibition of igf1r activation, inhibition of igf1-induced akt activation, but increased erk activation in nt157-treated cells. these effects were associated with decreased proliferation, increased apoptosis of lncap cells and increased g2-m arrest in pc3 cells. moreover, nt157 could significantly affect the cell migratory ability, as demonstrated by a wound-healing assay. in addition, the nt157 treatment was able to induce cell cycle arrest and inhibit igf system signaling [1].

• in vivo

  in previous animal study, nt157 was found to suppress androgen-responsive growth, delay crpc progression of lncap xenografts, and suppress pc3 tumor growth alone or in combination with docetaxel. this study reported the first preclinical proof-of-principle data that nt157 suppressed irs1/2 expression, delayed crpc progression, and suppressed growth of crpc tumors in vivo [1].

• IC 50

  0.3 to 0.8 μm

• Einzelnachweise

  [1] ibuki n et al. the tyrphostin nt157 suppresses insulin receptor substrates and augments therapeutic response of prostate cancer. mol cancer ther. 2014 dec;13(12):2827-39.

(E)-3-(3-bromo-4,5-dihydroxyphenyl)-N-(3,4,5-trihydroxybenzyl)prop-2-enethioamide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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