 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 1429639-50-8 |
| Molecular formula(MF) | C22H29N5O4S |
| Molecular Weight(MW): | 459.56 |
| Alias |
| In vitro | DMSO | 91 mg/mL (198.01 mM) |
|---|---|---|
| Water | <1 mg/mL | |
| Ethanol | <1 mg/mL | |
| In vivo |
| Description | CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability. | ||
|---|---|---|---|
| Targets |
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| In vitro |
CZ415 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[1]. |
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| In vivo | In 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 in vivo, CZ415 represents an ideal molecule for the pharmacological investigation of mTOR pathophysiological role in vivo[1]. |