Referencia número: HY-100222

CZ415

4 Cited Publications

Revisión del cliente

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.

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Pureza: 98.39%
No. CAS: 1429639-50-8
Fòrmula: C₂₂H₂₉N₅O₄S
Peso molecular:459.56

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CZ415 Chemical Structure

No. CAS: 1429639-50-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

CZ415 is a potent and highly selective mTOR inhibitor with a pIC₅₀ of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.

IC₅₀ & Target^[1]

mTOR

8.07 (pIC₅₀)

mTORC1

mTORC2

Ver todos los productos específicos de isoformas mTOR :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	48 μM Compound: 3; CZ415	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	[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

CZ415 is a highly selective mTOR inhibitor showing in vivo efficacy in a collagen induced arthritis (CIA) model. For full characterization of CZ415 and to enable improved dose predictions, the pharmacokinetic (PK) profile is assessed in rat. PK and oral bioavailability are determined after of 1 mg/kg intravenous (iv) bolus and 3 mg/kg oral (po) administration. The observed plasma clearance, corresponding to 45% liver blood flow, suggests that sufficient levels of free compound are circulating in the animal over time. The oral uptake is rapid with a T_maxmax of 0.5 h and bioavailability F = 44% indicates very good absorption from the gut^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 1429639-50-8
Appearance Solid
Peso molecular 459.56
Fòrmula C₂₂H₂₉N₅O₄S
Color White to off-white
SMILES

O=C(NCC)NC(C=C1)=CC=C1C2=NC3=C(CS(C3(C)C)(=O)=O)C(N4[C@@H](C)COCC4)=N2
Envío

Room temperature in continental US; may vary elsewhere.

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

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

ERK inhibition sensitizes CZ415-induced anti-osteosarcoma activity in vitro and in vivo. [Abstract]

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1760 mL

10.8800 mL

21.7599 mL

5 mM

0.4352 mL

2.1760 mL

4.3520 mL

10 mM

0.2176 mL

1.0880 mL

2.1760 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

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

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Cansfield AD, et al. CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model. ACS Med Chem Lett. 2016 Jun 10;7(8):768-73. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

CZ415

4 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) CZ415

Ver todos los productos específicos de isoformas mTOR

Actividad biológica

Chemical Information

Publications (4)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

CZ415 Related Classifications

HY-100222 Related Classifications