Art. -Nr.: HY-163199

ASCT2-IN-2

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ASCT2-IN-2 (compound 25e) is an ASCT2 inhibitor with IC₅₀ of 5.14 μM. ASCT2-IN-2 regulates amino acid metabolism as well as mTOR signaling and thereby induces cell apoptosis. ASCT2-IN-2 inhibits tumor growth.

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Reinheit: 99.10%
CAS. Nr.: 3032651-29-6
Formel: C₄₄H₅₀N₂O₄
Molecular Weight:670.88

Speicherung:

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

ASCT2-IN-2 Chemical Structure

CAS. Nr.: 3032651-29-6

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

Biologische Aktivität

Beschreibung

Alle ASCT Isoform-spezifische Produkte anzeigen :

ASCT2

Alle mTOR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	5.83 μM Compound: 25e	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 38217503]
NSCLC	IC₅₀	0.12 μM Compound: 25e	Antiproliferative activity against human NSCLC cells cultured as 2422 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay Antiproliferative activity against human NSCLC cells cultured as 2422 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay	[PMID: 38217503]
NSCLC	IC₅₀	1.09 μM Compound: 25e	Antiproliferative activity against human NSCLC cells cultured as H1975 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay Antiproliferative activity against human NSCLC cells cultured as H1975 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay	[PMID: 38217503]
NSCLC	IC₅₀	2.36 μM Compound: 25e	Antiproliferative activity against human NSCLC cells cultured as HCC827 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay Antiproliferative activity against human NSCLC cells cultured as HCC827 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay	[PMID: 38217503]
NSCLC	IC₅₀	2.85 μM Compound: 25e	Antiproliferative activity against human NSCLC cells cultured as 2862 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay Antiproliferative activity against human NSCLC cells cultured as 2862 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay	[PMID: 38217503]
NSCLC	IC₅₀	8.08 μM Compound: 25e	Antiproliferative activity against human NSCLC cells cultured as 2566 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay Antiproliferative activity against human NSCLC cells cultured as 2566 organoids assessed as cell viability incubated for 96 hrs by Celltiter-glo viability assay	[PMID: 38217503]

In Vitro

ASCT2-IN-2 (50 μM, 15 min) inhibits Glutamine (Gln) uptake in cells A549 and HEK293 (Gln inhibition ratio 55.62% and 98.31%) by targeting hASCT2, with IC₅₀ values of 5.6 μM and 3.5 μM, respectively^[1].
ASCT2-IN-2 (0-50 μM, 15 min) improves metabolic stability in murine liver microsome, with a half-time of 166.51 min and a clearance of 8.27 μL/min•mg^[1].
ASCT2-IN-2 (0-50 μM, 15 min) improves activity of LAT1 and thereby promotes leucine uptake in A549 cells^[1].
ASCT2-IN-2 (5-10 μM, 24 h) inhibits Gln metabolism, upregulates the ROS production and thereby induces apoptosis in cell A549^[1].
ASCT2-IN-2 (5-10 μM, 24 h) inhibits AKT phosphorylation and mTORC1 activity under starvation, promotes cell autophagy^[1].
ASCT2-IN-2 (5-10 μM, 24 h) dose-dependently inhibits proliferation in A549^[1].
ASCT2-IN-2 (0-10 nM, 96 h) inhibits organoid proliferation of drug resistant NSCLCs in cells H1975 OR and HCC827 OR ^[1].

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

Cell Viability Assay^[1]

Cell Line:

A549
Concentration:

50 μM
Incubation Time:

72 h
Result:

Exhibited antiproliferation activity in A549, with IC₅₀ of 5.83 μM.

In Vivo

ASCT2-IN-2 (i.p.;25 or 50 mg/kg, once every two days for 3 weeks) inhibits tumor growth with a TGI of 70% in A549 Xenograft Model in BALB/c mice^[1].

Pharmacokinetic Analysis of ASCT2-IN-2 in Sprague-Dawley rats^[1]

Route	Dose (mg/kg)	AUC_0→t (μg·h/L)	AUC_0→∞ (μg·h/L)	T_1/2 (h)	T_max (h)	C_max (ng/mL)	V/F(L/kg)	CL/F(L/h/kg)	MRT_0→∞(h)	Fr(%)
i.p.	10 mg/kg	13804.10	14544.59	19.41	5.33	874.32	19.99	0.72	20.73	396.73

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

Animal Model:

Tumor Growth in A549 Xenograft Model in BALB/c mice^[1]
Dosage:

25 and 50 mg/kg, once every two days for 3 weeks
Administration:

Intraperitoneal injection
Result:

Inhibited tumor growth with a TGI of 70%

Chemical Information

CAS. Nr. 3032651-29-6
Appearance Solid
Molecular Weight 670.88
Formel C₄₄H₅₀N₂O₄
Color White to off-white
SMILES

N[C@@H](CCN(CC1=C(C=CC(C(C)(C)C)=C1)OCC#CC2=CC=CC=C2)CC3=CC(C(C)(C)C)=CC=C3OCC#CC4=CC=CC=C4)C(O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 150 mg/mL (223.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

1.4906 mL

7.4529 mL

14.9058 mL

5 mM

0.2981 mL

1.4906 mL

2.9812 mL

10 mM

0.1491 mL

0.7453 mL

1.4906 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 (protect from light, stored under nitrogen). 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: ≥ 3.75 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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: ≥ 3.75 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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: ≥ 3.75 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 3.75 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 (37.5 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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]. Qin L et al., Discovery of Novel Aminobutanoic Acid-Based ASCT2 Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. J Med Chem. 2024 Jan 13. doi: 10.1021/acs.jmedchem.3c01093 [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4906 mL	7.4529 mL	14.9058 mL	37.2645 mL
	5 mM	0.2981 mL	1.4906 mL	2.9812 mL	7.4529 mL
	10 mM	0.1491 mL	0.7453 mL	1.4906 mL	3.7264 mL
	15 mM	0.0994 mL	0.4969 mL	0.9937 mL	2.4843 mL
	20 mM	0.0745 mL	0.3726 mL	0.7453 mL	1.8632 mL
	25 mM	0.0596 mL	0.2981 mL	0.5962 mL	1.4906 mL
	30 mM	0.0497 mL	0.2484 mL	0.4969 mL	1.2421 mL
	40 mM	0.0373 mL	0.1863 mL	0.3726 mL	0.9316 mL
	50 mM	0.0298 mL	0.1491 mL	0.2981 mL	0.7453 mL
	60 mM	0.0248 mL	0.1242 mL	0.2484 mL	0.6211 mL
	80 mM	0.0186 mL	0.0932 mL	0.1863 mL	0.4658 mL
	100 mM	0.0149 mL	0.0745 mL	0.1491 mL	0.3726 mL

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ASCT2-IN-2

Apoptosis Compound Library

Kinase Inhibitor Library

Membrane Transporter/Ion Channel Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Alkyne Compound Library

Alle ASCT Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ASCT2-IN-2 Related Classifications

HY-163199 Related Classifications