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CZ415

🥰Excellent
Catalog No. T3514Cas No. 1429639-50-8

CZ415 is a potent and highly selective mTOR inhibitor. This compound has a molecular weight of 432.51 g/mol and demonstrates an inhibition constant (IC50) of 5.8 nM against mTOR. Additionally, CZ415 has shown to be efficacious in preclinical models of cancer, indicating its potential therapeutic application in oncology.

CZ415

CZ415

🥰Excellent
Purity: 98.44%
Catalog No. T3514Cas No. 1429639-50-8
CZ415 is a potent and highly selective mTOR inhibitor. This compound has a molecular weight of 432.51 g/mol and demonstrates an inhibition constant (IC50) of 5.8 nM against mTOR. Additionally, CZ415 has shown to be efficacious in preclinical models of cancer, indicating its potential therapeutic application in oncology.
Pack SizePriceAvailabilityQuantity
1 mg$35In Stock
2 mg$47In Stock
5 mg$68In Stock
10 mg$112In Stock
25 mg$235In Stock
50 mg$355In Stock
100 mg$496In Stock
200 mg$687In Stock
1 mL x 10 mM (in DMSO)$69In Stock
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Purity:98.44%
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Product Introduction

Bioactivity
Description
CZ415 is a potent and highly selective mTOR inhibitor. This compound has a molecular weight of 432.51 g/mol and demonstrates an inhibition constant (IC50) of 5.8 nM against mTOR. Additionally, CZ415 has shown to be efficacious in preclinical models of cancer, indicating its potential therapeutic application in oncology.
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[1].
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].
Cell Research
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 (Only for Reference)
Chemical Properties
Molecular Weight459.56
FormulaC22H29N5O4S
Cas No.1429639-50-8
SmilesCCNC(=O)Nc1ccc(cc1)-c1nc2c(CS(=O)(=O)C2(C)C)c(n1)N1CCOC[C@@H]1C
Relative Density.1.287 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 84 mg/mL (182.8 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1760 mL10.8800 mL21.7599 mL108.7997 mL
5 mM0.4352 mL2.1760 mL4.3520 mL21.7599 mL
10 mM0.2176 mL1.0880 mL2.1760 mL10.8800 mL
20 mM0.1088 mL0.5440 mL1.0880 mL5.4400 mL
50 mM0.0435 mL0.2176 mL0.4352 mL2.1760 mL
100 mM0.0218 mL0.1088 mL0.2176 mL1.0880 mL

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