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CZ415

Catalog No. T3514   CAS 1429639-50-8

CZ415 is a potent and highly selective mTOR inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
CZ415 Chemical Structure
CZ415, CAS 1429639-50-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 59.00
5 mg In stock $ 117.00
10 mg In stock $ 187.00
25 mg In stock $ 392.00
50 mg In stock $ 592.00
100 mg In stock $ 845.00
1 mL * 10 mM (in DMSO) In stock $ 119.00
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Purity: 98.44%
Purity: 98.36%
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Biological Description
Chemical Properties
Storage & Solubility Information
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[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)
Molecular Weight 459.56
Formula C22H29N5O4S
CAS No. 1429639-50-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)

TargetMolReferences and Literature

1. Cansfield AD, et al. ACS Med Chem Lett. 2016, 7(8):768-73.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Anti-Cancer Metabolism Compound Library Metabolism Compound Library Stem Cell Differentiation Compound Library Anti-Pancreatic Cancer Compound Library Reprogramming Compound Library Oxidation-Reduction Compound Library Anti-Ovarian Cancer Compound Library Glycometabolism Compound Library PI3K-AKT-mTOR Compound Library

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Keywords

CZ415 1429639-50-8 PI3K/Akt/mTOR signaling mTOR inhibit Inhibitor CZ-415 Mammalian target of Rapamycin CZ 415 inhibitor

 

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