CZ415 /CAS:1429639-50-8

产品描述：CZ415 is a potent and highly selective mTOR inhibitor. IC50 & Target: mTOR^[1]
IC50: 14.5 nM (pS6RP), 14.8 nM (pAKT), 226 nM (IFNγ)^[1] In Vitro: Inhibition of phosphorylation for both downstream targets results in 14.5 nM IC₅₀ for pS6RP and 14.8 nM for pAKT. The immunosuppressive effect of CZ415 is measured by detecting secreted IFNγ after 18 hours in stimulated human whole blood and the resulting IC₅₀ is 226 nM. As a predictor for cardiotoxicity, the activity of CZ415 against the human cardiac ion channel hERG is assessed in a whole-cell patch-clamp assay in HEK293 cells resulting in an IC₅₀ of 48 μM^[1]. In Vivo: CZ415 is a highly selective mTOR inhibitor showing in vivo efficacy in a collagen induced arthritis (CIA) model. For full characterization of CZ415 and to enable improved dose predictions, the pharmacokinetic (PK) profile is assessed in rat. PK and oral bioavailability


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