5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H400：Sehr giftig für Wasserorganismen.

  H410：Sehr giftig für Wasserorganismen mit langfristiger Wirkung.

• Sicherheit

  P264：Nach Gebrauch gründlich waschen.

  P264：Nach Gebrauch gründlich waschen.

  P270：Bei Gebrauch nicht essen, trinken oder rauchen.

  P273：Freisetzung in die Umwelt vermeiden.

  P301+P312：BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

  P330：Mund ausspülen.

  P391：Verschüttete Mengen aufnehmen.

  P501：Inhalt/Behälter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  nms-e973 is a potent and selective inhibitor of heat shock protein 90 (hsp90) with dc50 value of < 10nm [1].since hsp90 plays an important role in the conformational maturation, stability and function of some oncogenic proteins, the inhibitors of hsp90 are developed as therapeutic for cancers. nms-e973 is a selective inhibitor of hsp90. it binds to hsp90α within the atp binding site with dc50 value of < 10nm. besides that, nms-e973 shows no effect on a panel of 52 various protein kinases such as abl, ack1, akt1 and alk. the ic50 value of it for hsc70 is > 10μm. nms-e973 exerts antiproliferation effects on a2780 tumor cell line and bt-474 breast cancer cell line with ic50 values of 69nm and 110nm, respectively. when treated with mice bearing a2780 xenografts, the intravenous administration of nms-e973 significantly inhibits tumor growth with tgi value of 53% at dose of 30mg/kg. moreover, nms-e973 also displays antitumor activity in tumors resistant to kinase inhibitors such as vemurafenib [1, 2].

• target

  Hsp90

• Einzelnachweise

  [1] brasca m g, mantegani s, amboldi n, et al. discovery of nms-e973 as novel, selective and potent inhibitor of heat shock protein 90 (hsp90). bioorganic & medicinal chemistry, 2013, 21(22): 7047-7063.
  [2] fogliatto g, gianellini l, brasca m g, et al. nms-e973, a novel synthetic inhibitor of hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases. clinical cancer research, 2013, 19(13): 3520-3532.

5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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