CZ415 is a potent and highly selective mTOR inhibitor.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 1 mg | In stock | $ 96 | |
| 2 mg | In stock | $ 182 | |
| 4 mg | In stock | $ 275 | |
| 10 mg | In stock | $ 552 | |
| 20 mg | In stock | $ 844 |
| Description | CZ415 is a potent and highly selective mTOR inhibitor. |
| Targets&IC50 | mTOR:8.07(pIC50) |
| 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. |
| 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. |
| CAS No. | 1429639-50-8 |
| Chemical Formula | C22H29N5O4S |
| Molecular Weight | 459.57 |
| Solubility | DMSO: 84 mg/mL (182.8 mM) H2O: <1 mg/mL; Ethanol: <1 mg/mL |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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