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

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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ASCT2-IN-1 Chemical Structure

ASCT2-IN-1 Chemical Structure

CAS No. : 3032651-18-3

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Based on 1 publication(s) in Google Scholar

ASCT2-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target

human ASCT2

3.5 μM (IC50)

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.

ASCT2-IN-1 Related Antibodies

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) 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 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%.
Molecular Weight

627.56

Formula

C36H32Cl2N2O4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°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 : 100 mg/mL (159.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5935 mL 7.9674 mL 15.9347 mL
5 mM 0.3187 mL 1.5935 mL 3.1869 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 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.

    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% 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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 1.5935 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 Related Classifications

Help & FAQs
  • 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.

Keywords:

ASCT2-IN-13032651-18-3ASCTmTORApoptosisAutophagyAlanine/serine/cysteine transporterMammalian target of RapamycinAntitumorA549HEK293BALB/c miceNSCLCInhibitorinhibitorinhibit

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