Cat. No.: HY-163198

ASCT2-IN-1

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ASCT2-IN-1 (compound 20k) is an ASCT2 inhibitor with IC₅₀ values of 5.6 μM and 3.5 μM in cells A549 and HEK293, respectively. ASCT2-IN-1 induces cell apoptosis. ASCT2-IN-1 inhibits tumor growth.

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Pureté: 98.21%
CAS No.: 3032651-18-3
Formule: C₃₆H₃₂Cl₂N₂O₄
Masse moléculaire:627.56

Stockage:

4°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-1 Chemical Structure

CAS No.: 3032651-18-3

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

human ASCT2

3.5 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform ASCT :

ASCT2

Voir tous les produits spécifiques à Isoform mTOR :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	10.35 μM Compound: 20k	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	22.43 μM Compound: 20k	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	5.09 μM Compound: 20k	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]
NSCLC	IC₅₀	5.21 μM Compound: 20k	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	7.34 μM Compound: 20k	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	8.45 μM Compound: 20k	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]

In Vitro

ASCT2-IN-1 (50 μM,15 min) inhibits Gln uptake in cells A549 and HEK293 by targeting hASCT2, with IC₅₀ values of 5.6 μM and 3.5 μM, respectively^[1].
ASCT2-IN-1 (0-50 μM, 15 min) improved metabolic stability in murine liver microsome, with a half-time of 37.15 min and a clearance of 37.48 μL/min•mg^[1].
ASCT2-IN-1 (0-50 μM, 15 min) inhibits amino acid transporter SNAT2 in cells A549 as well as transporter LAT1 in overexpressing HEK293 ^[1].
ASCT2-IN-1 (5-10 μM, 24 h) inhibits Gln metabolism, upregulates the ROS production and thereby induces apoptosis in cell A549^[1].
ASCT2-IN-1 (5-10 μM, 24 h) inhibits AKT phosphorylation and mTORC1 activity under starvation, promotes cell autophagy^[1].
ASCT2-IN-1 (5-10 μM, 24 h) dose-dependently inhibits proliferation in A549^[1].
ASCT2-IN-1 (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.

Western Blot Analysis^[1]

Cell Line:

A549
Concentration:

5 and 10 μM
Incubation Time:

24 h
Result:

Activated Caspase reaction and induced apoptosis.

Western Blot Analysis^[1]

Cell Line:

A549
Concentration:

5 and 10 μM
Incubation Time:

24 h
Result:

Decreased mTORC1 and phosphorylarion of AKT.

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 65% in NSCLC xenograft model in BALB/c mice ^[1].

Pharmacokinetic Analysis of ASCT2-IN-1 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	2674.95	2824.42	9.41	1.17	323.07	49.54	3.63	13.69	77.04

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

Animal Model:

NSCLC Xenograft model in BALB/c nude mice ^[1]
Dosage:

25, 50 mg/kg
Administration:

Intraperitoneal injection, once every two days for 3 weeks
Result:

Inhibited tumor growth with TGI of 65%.

Chemical Information

CAS No. 3032651-18-3
Appearance Solid
Masse moléculaire 627.56
Formule C₃₆H₃₂Cl₂N₂O₄
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light, stored under nitrogen

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

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (159.35 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

1.5935 mL

7.9674 mL

15.9347 mL

5 mM

0.3187 mL

1.5935 mL

3.1869 mL

10 mM

0.1593 mL

0.7967 mL

1.5935 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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 (3.98 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.98 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (252 KB)
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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)
Instruction de manipulation (2659 KB)

Références

[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	1.5935 mL	7.9674 mL	15.9347 mL	39.8368 mL
	5 mM	0.3187 mL	1.5935 mL	3.1869 mL	7.9674 mL
	10 mM	0.1593 mL	0.7967 mL	1.5935 mL	3.9837 mL
	15 mM	0.1062 mL	0.5312 mL	1.0623 mL	2.6558 mL
	20 mM	0.0797 mL	0.3984 mL	0.7967 mL	1.9918 mL
	25 mM	0.0637 mL	0.3187 mL	0.6374 mL	1.5935 mL
	30 mM	0.0531 mL	0.2656 mL	0.5312 mL	1.3279 mL
	40 mM	0.0398 mL	0.1992 mL	0.3984 mL	0.9959 mL
	50 mM	0.0319 mL	0.1593 mL	0.3187 mL	0.7967 mL
	60 mM	0.0266 mL	0.1328 mL	0.2656 mL	0.6639 mL
	80 mM	0.0199 mL	0.0996 mL	0.1992 mL	0.4980 mL
	100 mM	0.0159 mL	0.0797 mL	0.1593 mL	0.3984 mL

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ASCT2-IN-1

Apoptosis Compound Library

Kinase Inhibitor Library

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Lactylation Compound Library

Alkyne Compound Library

Voir tous les produits spécifiques à Isoform ASCT

Voir tous les produits spécifiques à Isoform mTOR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ASCT2-IN-1 Related Classifications

HY-163198 Related Classifications