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ASCT2-IN-1

Catalog No.GC74029

ASCT2-IN-1 (composé 20k) est un inhibiteur d’asct2 avec des valeurs de ci50 de 5,6 μM et 3,5 μM dans les cellules A549 et HEK293, respectivement.

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ASCT2-IN-1 Chemical Structure

Cas No.: 3032651-18-3

Taille Prix Stock Qté
1 mg
113,00 $US
En stock
5 mg
279,00 $US
En stock
10 mg
450,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Description of 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.

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].

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]

References:
[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

Chemical Properties of ASCT2-IN-1

Cas No. 3032651-18-3 SDF
Formula C36H32Cl2N2O4 M.Wt 627.56
Solubility DMSO : 100 mg/mL (159.35 mM; Need ultrasonic) Storage 4°C, protect from light, stored under nitrogen
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of ASCT2-IN-1

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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
10 mM 0.1593 mL 0.7967 mL 1.5935 mL
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