Home Transmembrane Transporters Amino acid transporter antagonist V-9302 For research use only.

V-9302

V-9302 is a competitive small molecule antagonist of transmembrane glutamine flux, that selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) with an IC50 value of 9.6 μM for inhibition of glutamine uptake in HEK-293 cells. V-9302 blocks Sodium-neutral AA transporter 2 (SNAT2, SLC38A2) and the large neutral AA transporter 1 (LAT1, SLC7A5) as observed in 143B osteosarcoma cells, HCC1806 breast cancer cells and Xenopus laevis oocytes. Dilution of PBS may cause a clear aqueous solution to turn into a uniform suspension.

V-9302 Chemical Structure

V-9302 Chemical Structure

CAS No. 1855871-76-9

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V-9302 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C6 Function assay Inhibition of ASCT2-mediated glutamine transport in rat C6 cells using [3H]-glutamine after 15 mins by scintillation counting, IC50 = 9 μM. 26750251
HEK293 Function assay Inhibition of ASCT2-mediated glutamine transport in human HEK293 cells using [3H]-glutamine after 15 mins by scintillation counting, IC50 = 9.6 μM. 26750251
Click to View More Cell Line Experimental Data

Biological Activity

Description V-9302 is a competitive small molecule antagonist of transmembrane glutamine flux, that selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) with an IC50 value of 9.6 μM for inhibition of glutamine uptake in HEK-293 cells. V-9302 blocks Sodium-neutral AA transporter 2 (SNAT2, SLC38A2) and the large neutral AA transporter 1 (LAT1, SLC7A5) as observed in 143B osteosarcoma cells, HCC1806 breast cancer cells and Xenopus laevis oocytes. Dilution of PBS may cause a clear aqueous solution to turn into a uniform suspension.
Targets
ASCT2 [1]
(HEK293 cells)
9.6 μM
In vitro
In vitro

V-9302 inhibits ASCT2-mediated glutamine uptake in human cells in a concentration-dependent fashion and exhibits a 100-fold improvement in potency (IC50 V-9302 = 9.6 µM) over gamma-L-glutamyl-p-nitroanilide (GPNA; IC50 = 1000 µM)[1].
Cell Research Cell lines HCC1806 cells
Concentrations 25 µM
Incubation Time 48 h
Method

HCC1806 cells are treated V-9302 (25 µM aqueous, 1% DMSO) for 48 h. Following treatment, cells are fixed with 70% methanol for 5-10 min. LC3B is visualized with 1:100 primary antibody at 37 ºC for 45 min followed by application of 1:600 secondary antibody at 37 ºC for 30 min and DAPI for 4 min.
Experimental Result Images Methods Biomarkers Images PMID
Western blot ASCT2 / pS6 / S6 / pERK / ERK 29334372
Growth inhibition assay Cell viability 29334372
In Vivo
In vivo

Pharmacological blockade of ASCT2 with V-9302 results in attenuated cancer cell growth and proliferation, increases cell death, and increases oxidative stress, which collectively, contributes to anti-tumor responses in vitro and in murine models in vivo. The steady-state plasma concentrations are achieved 4 h post-administration, with a half-life of approximately 6 h in healthy mice. Following a single acute V-9302 exposure (4 h), plasma glucose levels are not significantly different than vehicle controls, yet plasma glutamine levels are elevated by approximately 50% in V-9302-treated mice compared to vehicle controls, likely a pharmacodynamic effect. Plasma glucose levels in mice chronically exposed to V-9302 or vehicle over a 21-day regimen are not significantly different, while plasma glutamine levels are slightly decreased[1].
Animal Research Animal Models cell-line xenograft tumors (propagated in 6-week old, female athymic nude mice)
Dosages 75 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 538.68 Formula

C34H38N2O4
CAS No. 1855871-76-9 SDF --
Smiles CC1=CC(=CC=C1)COC2=CC=CC=C2CN(CCC(C(=O)O)N)CC3=CC=CC=C3OCC4=CC=CC(=C4)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (185.63 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
What should be done if the water soluble mother liquor of S8818 becomes cloudy when diluted into cell medium or PBS solution?

Answer:
During cell experiments, the mother liquor prepared with pure water may temporarily become turbid after adding PBS. It can be clarified again by standing at room temperature for half an hour. For animal experiments, please directly use PBS to prepare drugs.

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