V-9302

Catalog No.S8818

For research use only.

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.

V-9302 Chemical Structure

CAS No. 1855871-76-9

Selleck's V-9302 has been cited by 8 Publications

Purity & Quality Control

Choose Selective Amino acid transporter Inhibitors

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.
Targets
ASCT2 [1]
(HEK293 cells)
9.6 μM
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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C6 MUHGeY5kfGmxbjDhd5NigQ>? MoHXTY5pcWKrdHnvckBw\iCDU1PUNk1u\WSrYYTl[EBodHW2YX3pcoUhfHKjboPwc5J1KGmwIILheEBEPiClZXzsd{B2e2mwZzDbN2heNWeudYThcYlv\SCjZoTldkAyPSCvaX7zJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTBiPTC5JO69VS5? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd3MEK1NUc,OjZ5NUCyOVE9N2F-
HEK293 NIj2OpJHfW6ldHnvckBie3OjeR?= MnPJTY5pcWKrdHnvckBw\iCDU1PUNk1u\WSrYYTl[EBodHW2YX3pcoUhfHKjboPwc5J1KGmwIHj1cYFvKEiHS{K5N{Bk\WyuczD1d4lv\yCdM1jdMYdtfXSjbXnu[UBi\nSncjCxOUBucW6|IHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVAhRSB7Lk[g{txONg>? NHXwbok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke1NFI2OSd-Mk[3OVAzPTF:L3G+
Assay
Methods Test Index PMID
Western blot ASCT2 / pS6 / S6 / pERK / ERK 29334372
Growth inhibition assay Cell viability 29334372
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].

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: cell-line xenograft tumors (propagated in 6-week old, female athymic nude mice)
  • Dosages: 75 mg/kg
  • Administration: IP

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 538.68
Formula

C34H38N2O4

CAS No. 1855871-76-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=CC=C1)COC2=CC=CC=C2CN(CCC(C(=O)O)N)CC3=CC=CC=C3OCC4=CC=CC(=C4)C

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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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