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V-9302 is a potent, selective small molecule antagonist of the amino acid transporter ASCT2 (also known as SLC1A5). It competitively inhibits transmembrane glutamine flux by blocking ASCT2-mediated glutamine uptake (IC50 ≈ 9.6 µM in human cells), leading to metabolic stress in cancer cells. This inhibition results in decreased mTOR activity, increased autophagy, and elevated oxidative stress, ultimately reducing cell viability and tumor growth in preclinical models. V-9302 is primarily being investigated as an anti-cancer agent due to its ability to disrupt glutamine metabolism—a key vulnerability in many tumors[1][5][7].
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