Home PI3K/Akt/mTOR mTOR inhibitor CZ415 For research use only.

CZ415

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

CZ415 Chemical Structure

CZ415 Chemical Structure

CAS: 1429639-50-8

Purity & Quality Control

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

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Signaling Pathway

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Biological Activity

Description CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability.
Targets
mTOR [1]
(Cell-free assay)
8.07(pIC50)
In vitro
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].
Cell Research Cell lines HEK294T17 cells
Concentrations 3 µM start, 8 points 1:3 dilution steps.
Incubation Time 2 h
Method Cells are seeded in 90 µL DMEM containing 2% FCS at 4x104 cells/well (for pS6RP S240/244 assay) or 8x104 cells/well (for pAKT S473 assay) in a 96well U-bottom plate. The plate is then incubated for 1h in a humidified incubator (37ºC, 5% CO2) to allow cells to adhere. CZ415: 3 µM start, 8 points 1:3 dilution steps, n=2. Positive control: 1 μM PI-103 (n=8). Negative control: DMSO (n=8). 10 µL of 10x compound concentration in 1% DMSO/99% (DMEM 2% FCS) are added to the cells followed by 2 h incubation in a humidified incubator (37ºC, 5% CO2). Cells are lysed by addition of 10 μL 5x Complete Lysis Buffer and gentle shaking at 4°C for 15 min
In Vivo
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].
Animal Research Animal Models Male SD rats
Dosages 1 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 459.56 Formula

C22H29N5O4S
CAS No. 1429639-50-8 SDF Download CZ415 SDF
Smiles CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CS(=O)(=O)C3(C)C)C(=N2)N4CCOCC4C
Storage (From the date of receipt)

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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