Home PI3K/Akt/mTOR mTOR inhibitor CZ415

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CZ415 mTOR inhibitor

Cat.No.S8298

CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability.
CZ415 mTOR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 459.56

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Quality Control

Batch: S829801 DMSO]91 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.32%
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99.32

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (198.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 459.56 Formula

C22H29N5O4S

 Storage (From the date of receipt)
CAS No. 1429639-50-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CS(=O)(=O)C3(C)C)C(=N2)N4CCOCC4C

Mechanism of Action

Targets/IC50/Ki
mTOR
(Cell-free assay)
8.07(pIC50)
In vitro
CZ415 shows no genotoxic potential and has very good cell permeability. Treatment of this compound 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 this compound is measured by detecting secreted IFNγ after 18 h in stimulated human whole blood, and the resulting IC50 was 226 nM. It 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 this compound 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, this molecule represents an ideal candidate for the pharmacological investigation of mTOR pathophysiological role in vivo.
References

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