Home PI3K/Akt/mTOR mTOR inhibitor CZ415

research use only

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

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

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

Solubility

In vitro
Batch:

DMSO : 91 mg/mL ( (198.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
mTOR [1]
(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[1].
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[1].
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Signaling Pathway Map