NVP-BEP800

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H317：Kann allergische Hautreaktionen verursachen.

  H319：Verursacht schwere Augenreizung.

• Sicherheit

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

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

NVP-BEP800 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Verwenden

  NVP-BEP 800 is a Hsp90 inhibitor which ehibits anti-proliferative effects against cancer cell lines with high expression level of Hsp90.

• Biologische Aktivität

  nvp-bep800 is a fully synthetic, orally bioavailable inhibitor of hsp90 with ic50 value of 58nm [1].nvp-bep800 binds to the n-terminal atp-binding pocket of hsp90. in a competitive binding fluorescence polarization assay, nvp-bep800 inhibits hsp90β with ic50 value of 58nm. and to other 20 protein kinases, nvp-bep800 shows a ic50 of >10μm. in bt-474 cells and a375 cells, nvp-bep800 causes the hsp90-p23 dissociation and client protein degradation (erbb2) as well as the reduction of client protein phosphorylation (phospho-akt). degradation of these oncogenic client proteins results in tumor cell growth arrest and death. nvp-bep800 inhibits proliferation of tumor cells with an average gi50 of 245nm. and in 46 primary human tumors including small cell lung, mammary cancer and melanoma, the mean ic50 is 750nm. additionally, treatment of nvp-bep800 induces apoptosis in human breast cancer cell lines. the antitumor efficacy of nvp-bep800 is also observed with a dose of 15 or 30 mg/kg/d in a375 xenograft-bearing mice as well as in bt-474 breast cancer xenografts [1].

• target

  Hsp90β

• Einzelnachweise

  [1] massey aj, schoepfer j, brough pa, brueggen j, chène p, drysdale mj, pfaar u, radimerski t, ruetz s, schweitzer a, wood m, garcia-echeverria c, jensen mr. preclinical antitumor activity of the orally available heat shock protein 90 inhibitor nvp-bep800. mol cancer ther. 2010 apr;9(4):906-19.

NVP-BEP800 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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