V-9302

Catalog No.S8818 Batch:S881801

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Technical Data

Formula

C34H38N2O4
Molecular Weight 538.68 CAS No. 1855871-76-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (185.63 mM)
Water 100 mg/mL (185.63 mM)
Ethanol 100 mg/mL (185.63 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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].
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 Assay:

[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 Study:

[1]
  • Animal Models

    cell-line xenograft tumors (propagated in 6-week old, female athymic nude mice)

  • Dosages

    75 mg/kg

  • Administration

    IP

Selleck's V-9302 has been cited by 13 publications

Targeting metabolic adaptive responses induced by glucose starvation inhibits cell proliferation and enhances cell death in osimertinib-resistant non-small cell lung cancer (NSCLC) cell lines [ Biochem Pharmacol, 2024, S0006-2952(24)00144-8] PubMed: 38522556
Mesothelioma cancer cells are glutamine addicted and glutamine restriction reduces YAP1 signaling to attenuate tumor formation [ Mol Carcinog, 2023, 62(4):438-449] PubMed: 36562471
Neddylation inhibition induces glutamine uptake and metabolism by targeting CRL3SPOP E3 ligase in cancer cells [ Nat Commun, 2022, 13(1):3034] PubMed: 35641493
Mapping of functional SARS-CoV-2 receptors in human lungs establishes differences in variant binding and SLC1A5 as a viral entry modulator of hACE2 [ EBioMedicine, 2022, 87:104390] PubMed: 36584595
PET/MR Imaging of a Lung Metastasis Model of Clear Cell Renal Cell Carcinoma with (2S,4R)-4-[18F]Fluoroglutamine [ Mol Imaging Biol, 2022, 10.1007/s11307-022-01747-9] PubMed: 35732988
Targeting of the glutamine transporter SLC1A5 induces cellular senescence in clear cell renal cell carcinoma [ Biochem Biophys Res Commun, 2022, 611:99-106] PubMed: 35487063
Evaluation of Glutaminolysis in T Cells [ Curr Protoc, 2022, 2(9):e540] PubMed: 36111948
Metabolic stress induces GD2+ cancer stem cell-like phenotype in triple-negative breast cancer [ Br J Cancer, 2021, 10.1038/s41416-021-01636-y] PubMed: 34811508
Oncogenic KRAS mutations enhance amino acid uptake by colorectal cancer cells via the hippo signaling effector YAP1 [ Mol Oncol, 2021, 10.1002/1878-0261.12999] PubMed: 34003553
Oncogenic KRAS mutations enhance amino acid uptake by colorectal cancer cells via the hippo signaling effector YAP1 [ Mol Oncol, 2021, 10.1002/1878-0261.12999] PubMed: 34003553

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.