CZ415
Based on 4 publication(s) in Google Scholar
CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.07%
- No. CAS: 1429639-50-8
- Fòrmula: C22H29N5O4S
- Peso molecular:459.56
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CZ415
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
mTOR 8.07 (pIC50) |
mTORC1 |
mTORC2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
48 μM
Compound: 3; CZ415
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Inhibition of human ERG expressed in HEK293 cells by whole cell patch clamp assay
Inhibition of human ERG expressed in HEK293 cells by whole cell patch clamp assay
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[PMID: 27563401] |
In Vitro
Inhibition of phosphorylation for both downstream targets results in 14.5 nM IC50 for pS6RP and 14.8 nM for pAKT. The immunosuppressive effect of CZ415 is measured by detecting secreted IFNγ after 18 hours in stimulated human whole blood and the resulting IC50 is 226 nM. As a predictor for cardiotoxicity, the activity of CZ415 against the human cardiac ion channel hERG is assessed in a whole-cell patch-clamp assay in HEK293 cells resulting in an IC50 of 48 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1429639-50-8
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Appearance Solid
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Peso molecular 459.56
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Fòrmula C22H29N5O4S
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Color White to off-white
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SMILES
O=C(NCC)NC(C=C1)=CC=C1C2=NC3=C(CS(C3(C)C)(=O)=O)C(N4[C@@H](C)COCC4)=N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell
Innate immune and metabolic signals induce mitochondria-dependent membrane lysis via mitoxyperiosis. [Abstract]2025 Dec 11;188(25):7155-7174.e25. PMID: 41317732 -
Front Pharmacol
CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]2020 Nov 11:11:580407. PMID: 33343350 -
Acta Trop
Tacrolimus, a rapamycin target protein inhibitor, exerts anti-cystic echinococcosis effects both in vitro and in vivo. [Abstract]2020 Dec:212:105708. PMID: 32956634 -
Oncotarget
2017 May 30;8(47):82027-82036. PMID: 29137241
CZ415 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 May 30;8(47):82027-82036. [Abstract]
U0126 and MEK162 block ERK activation (p-ERK1/2) in CZ415-treated U2OS cells.
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (217.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Animal Administration[1]
Mice[1]
To determine the effects of CZ415 on its pharmacological target, dose-dependent changes in phosphorylation levels of S6 Ribosomal Protein and Akt - both downstream targets of mTOR are assessed. CZ415 is administered orally at 1, 3 and 10 mg/kg to mice 1 h before anti-CD3 stimulus. 15 min after stimulation, spleens are dissected and analyzed for pS6RP and pAKT levels. A dose related significant inhibition of phosphorylation of both S6RP and Akt are observed after compound administration. In particular, 1 and 3 mg/kg CZ415 could fully inhibit S6RP phosphorylation induced by anti-CD3 stimulation and 10 mg/kg additionally decreased the constitutive phosphorylation levels as measured in the control group.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1760 mL | 10.8800 mL | 21.7599 mL | 54.3999 mL |
| 5 mM | 0.4352 mL | 2.1760 mL | 4.3520 mL | 10.8800 mL | |
| 10 mM | 0.2176 mL | 1.0880 mL | 2.1760 mL | 5.4400 mL | |
| 15 mM | 0.1451 mL | 0.7253 mL | 1.4507 mL | 3.6267 mL | |
| 20 mM | 0.1088 mL | 0.5440 mL | 1.0880 mL | 2.7200 mL | |
| 25 mM | 0.0870 mL | 0.4352 mL | 0.8704 mL | 2.1760 mL | |
| 30 mM | 0.0725 mL | 0.3627 mL | 0.7253 mL | 1.8133 mL | |
| 40 mM | 0.0544 mL | 0.2720 mL | 0.5440 mL | 1.3600 mL | |
| 50 mM | 0.0435 mL | 0.2176 mL | 0.4352 mL | 1.0880 mL | |
| 60 mM | 0.0363 mL | 0.1813 mL | 0.3627 mL | 0.9067 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2720 mL | 0.6800 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5440 mL |
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