CC-115

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• 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.

CC-115 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  cc-115 is a inhibitor of mtor/dna-pk.the mammalian target of rapamycin (mtor) kinase is a key mediator of the phosphoinositide 3-kinase /protein kinase b (akt pathway). the dna-dependent protein kinase (dna-pk) is a critical component of the dna repair machinery governings the response to dna damage, which serves to maintain genome integrity.

• in vitro

  previous study found that the proliferation induced by cd40(+) interleukin-21 stimulation could be completely blocked by cc-115, and cd40-mediated resistance to fludarabine and venetoclax could also be reverted by cc-115. moreover, bcr-mediated signaling was blocked by cc-115 and in cll samples from patients with acquired resistance to idelalisib treatment [1].

• in vivo

  preclinical studies showed that cc-115 had good in vivo pk profiles across multiple species with 53%, 76%, and around100% oral bioavailability in mouse, rat, and dog, respectively [2].

• target

  Target	Value
  DNA-PK (Cell-free assay)	0.013 μM
  mTOR (Cell-free assay)	0.021 μM
  PI3Kα (Cell-free assay)	0.852 μM

• IC 50

  21/ 13 nm for mtor/dna-pk

• Einzelnachweise

  [1] thijssen r,et al. dual tork/dna-pk inhibition blocks critical signaling pathways in chronic lymphocytic leukemia. blood.2016 jul 28;128(4):574-83.
  [2] mortensen ds, et al. optimization of a series of triazole containing mammalian target of rapamycin (mtor) kinase inhibitors and the discovery of cc-115. j med chem. 2015 jul 23;58(14):5599-5608.

CC-115 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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