INDEX NAME NOT YET ASSIGNED

INDEX NAME NOT YET ASSIGNED Chemische Eigenschaften,Einsatz,Produktion Methoden

• Verwenden

  OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively. OTUB1/USP8-IN-1 can be used in research of cancer[1].

• in vivo

  OTUB1/USP8-IN-1 (compound 61; 10 nM-10 μM; 72 h) decreases the tumor burden in the H1975 xenograft mouse model^[1].

  Animal Model:	Female BALB/c nude mice with H1975 xenografts (5 weeks of age)[1]
  Dosage:	5 mg/kg
  Administration:	Intraperitoneal injection; QD and BID, for 2 weeks
  Result:	Reduced total tumor weight and average tumor volume in an over twofold with BID dosing.

  Animal Model:	Female BALB/c nude mice with H1975 xenograft (5 weeks of age)[1]
  Dosage:	1 and 10 mg/kg
  Administration:	Intravenous injection (1 mg/kg) and oral administration (10 mg/kg)
  Result:	1.19 Administration i.v. (1 mg/kg) p.o. (10 mg/kg) T1/2 (h) 0.83 1.75 Tmax (h) 0.33 Cmax (μg/L) 4274 AUC (μg·h/L) 1345 3747 CL (L/h/kg) 44 Vdss (L/kg) 0.77

• Einzelnachweise

  [1] Tan L, et, al. Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. J Med Chem. 2022 Oct 11. DOI:10.1021/acs.jmedchem.2c00408

INDEX NAME NOT YET ASSIGNED Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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