1. Membrane Transporter/Ion Channel PI3K/Akt/mTOR Apoptosis Autophagy
  2. ASCT mTOR Apoptosis Autophagy
  3. ASCT2-IN-2

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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ASCT2-IN-2 Chemical Structure

ASCT2-IN-2 Chemical Structure

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5 mg USD 280 In-stock
10 mg USD 450 In-stock
25 mg USD 930 In-stock
50 mg USD 1500 In-stock
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Description

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[1].

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) AUC0→t (μg·h/L) AUC0→∞ (μg·h/L) T1/2 (h) Tmax (h) Cmax (ng/mL) V/F(L/kg) CL/F(L/h/kg) MRT0→∞(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%
Molecular Weight

670.88

Formula

C44H50N2O4

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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

Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4906 mL 7.4529 mL 14.9058 mL
5 mM 0.2981 mL 1.4906 mL 2.9812 mL
View the 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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, 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.

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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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ASCT2-IN-2
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HY-163199
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