CZ415 (C09-0823-257)

InformationCZ415 CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability.TargetsmTOR (Cell-free assay) 8.07(pIC50)In vitroCZ415 shows no genotoxic potential and has very good cell permeability. Treatment of CZ415 leads to inhibition of phosphorylation for downstream targets of mTORC1 and mTORC2(IC50=14.5 nM for pS6RP and IC50=14.8 nM for pAKT). The immunosuppressive effect of CZ415 is measured by detecting secreted IFNγ after 18 h in stimulated human whole blood, and the resulting IC50 was 226 nM. CZ415 shows no genotoxic potential. It is neither mutagenic in a bacterial mutation assay (Ames test) nor does it show genotoxicity in the mouse lymphoma assay (MLA), in either the presence or absence of rat-liver S9 mix.In vivoIn vivo studies show that CZ415 has moderate clearance and good oral bioavailability. In an anti-CD3 mouse model CZ415 efficiently inhibits mTOR downstream signaling and, in a CIA mouse model, shows significant antiinflammatory effects. With its extraordinary selectivity, drug-like properties and proven efficacy CZ415 represents an ideal molecule for the pharmacological investigation of mTOR pathophysiological role in vivo.Cell Research(from reference)Cell lines：HEK294T17 cells Concentrations：3 µM start, 8 points 1:3 dilution steps. Incubation Time：2 h. Specification: 0.98 Molecular Formula: C22H29N5O4S Molecular Weight: 459.56 PubChem CID: 71547699 Isomeric SMILES: CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CS(=O)(=O)C3(C)C)C(=N2)N4CCOC[C@@H]4C Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/C413966-SCI_bfca378550d53a55cfc103a5d997cb98.pdf