2. PI3K/Akt/mTOR Apoptosis Autophagy
  3. 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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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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ASCT2-IN-1 Related Classifications

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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-13032651-18-3mTORApoptosisAutophagyMammalian target of RapamycinAntitumorA549HEK293BALB/c miceNSCLCInhibitorinhibitorinhibit

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