Art. -Nr.: HY-131344

mTOR inhibitor-8

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mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.

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Reinheit: 98.14%
CAS. Nr.: 2489196-70-3
Formel: C₂₄H₁₉ClN₄OS
Molecular Weight:446.95

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

mTOR inhibitor-8 Chemical Structure

CAS. Nr.: 2489196-70-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells^[1].

IC₅₀ & Target^[1]

mTOR

Autophagy

Alle mTOR Isoform-spezifische Produkte anzeigen :

In Vitro

mTOR inhibitor-8 (Compound 5e; 0.1-10 μM; 24 and 48 hours) suppresses the growth of A549 cells in a dose-dependent manner^[1].
mTOR inhibitor-8 induces autophagy in an mTOR-dependent manner. mTOR inhibitor-8 (10 μM; 3-24 hours) induces autophagy in a time-dependent manner. The levels of LC3B-II are enhanced^[1].
mTOR inhibitor-8 (10 μM; 3-24 hours) reduces the phosphorylation of RPS6KB1 (ribosomal protein S6 kinase) and EIF4EBP1 (eukaryotic translation initiation factor 4E-binding protein 1), two essential substrates of mTOR^[1]

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

Cell Viability Assay^[1]

Cell Line:

A549 cells
Concentration:

0.1, 1, 5, 10 μM
Incubation Time:

24 and 48 hours
Result:

Suppressed the growth of A549 cells with an IC₅₀ of 2.6±0.11 μM.

Western Blot Analysis^[1]

Cell Line:

A549 cells
Concentration:

10 μM
Incubation Time:

3, 6, 12 and 24 hours
Result:

The levels of phosphorylation of RPS6KB1 and EIF4EBP1 were significantly decreased after treatment.

In Vivo

mTOR inhibitor-8 (25 and 50 μM; 6 days) effectively inhibits tumor growth in vivo without adverse effect on normal chick chorioallantoic membrane angiogenesis^[1].

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

Animal Model:

Fertile chicken eggs (7-9 days old)^[1]
Dosage:

25 and 50 μM
Administration:

6 days
Result:

Significant xenograft tumor remission was observed in eggs compared with the DMSO-treated eggs.

Chemical Information

CAS. Nr. 2489196-70-3
Appearance Solid
Molecular Weight 446.95
Formel C₂₄H₁₉ClN₄OS
Color White to yellow
SMILES

COC1=CC=C(C2CC(C3=CC=C(Cl)C=C3)=NN2C4=NC(C5=CC=NC=C5)=CS4)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 31.25 mg/mL (69.92 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

2.2374 mL

11.1869 mL

22.3739 mL

5 mM

0.4475 mL

2.2374 mL

4.4748 mL

10 mM

0.2237 mL

1.1187 mL

2.2374 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: 2.08 mg/mL (4.65 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Handling Instructions (2659 KB)

Verweise

[1]. ZhaoMin Lin, et al. Discovery of new fluorescent thiazole-pyrazoline derivatives as autophagy inducers by inhibiting mTOR activity in A549 human lung cancer cells. Cell Death Dis. 2020 Jul 20;11(7):551. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2374 mL	11.1869 mL	22.3739 mL	55.9347 mL
	5 mM	0.4475 mL	2.2374 mL	4.4748 mL	11.1869 mL
	10 mM	0.2237 mL	1.1187 mL	2.2374 mL	5.5935 mL
	15 mM	0.1492 mL	0.7458 mL	1.4916 mL	3.7290 mL
	20 mM	0.1119 mL	0.5593 mL	1.1187 mL	2.7967 mL
	25 mM	0.0895 mL	0.4475 mL	0.8950 mL	2.2374 mL
	30 mM	0.0746 mL	0.3729 mL	0.7458 mL	1.8645 mL
	40 mM	0.0559 mL	0.2797 mL	0.5593 mL	1.3984 mL
	50 mM	0.0447 mL	0.2237 mL	0.4475 mL	1.1187 mL
	60 mM	0.0373 mL	0.1864 mL	0.3729 mL	0.9322 mL

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mTOR inhibitor-8

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Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

mTOR inhibitor-8 Related Classifications

HY-131344 Related Classifications