1. PI3K/Akt/mTOR Apoptosis Autophagy
  2. 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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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

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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References
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ASCT2-IN-2 Related Classifications

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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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