| Identification | Back Directory | [Name]
V-9302 HCl | [CAS]
2416138-42-4 | [Synonyms]
(S)-2-Amino-4-(bis(2-((3-methylbenzyl)oxy)benzyl)amino)butanoic acid hydrochloride | [Molecular Formula]
C34H39ClN2O4 | [MOL File]
2416138-42-4.mol | [Molecular Weight]
575.15 |
| Hazard Information | Back Directory | [Uses]
V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 μM) in HEK-293 cells[1]. | [in vivo]
V-9302 hydrochloride (75 mg/kg; i.p.; daily fo 21 days) prevents tumor growth in both HCT-116 and HT29 xenograft models[1].
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The combination of? CB-839 and V-9302 (30 mg/kg; i.p.; SNU398 and MHCC97H cells were grown as tumor xenografts in BALB/c nude mice; for 20 or 15 d, respectively) elicits a strong growth inhibition in both SNU398 and MHCC97H xenograft models, while single-drug treatment showed modest anti-tumor effects[2].
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V-9302 (50 mg/kg ; i.p.; daily for 5 days) displays markedly reduced tumor growth[3]. | Animal Model: | 6-week old, female athymic nude mice (bearing HCT-116 (KRASG13D) or HT29 (BRAFV600E) cell-line )[1] | | Dosage: | 75 mg/kg | | Administration: | Intraperitoneally; daily fo 21 days
| | Result: | Prevented tumor growth.
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| [IC 50]
ASCT2 | [References]
[1] Schulte ML, et al. Pharmacological blockade of ASCT2-dependent glutamine transport leads to antitumor efficacyin preclinical models. Nat Med. 2018 Feb;24(2):194-202. DOI:10.1038/nm.4464
[2] Jin H, et al. A powerful drug combination strategy targeting glutamine addiction for the treatment of human liver cancer. Elife. 2020;9:e56749. Published 2020 Oct 5. DOI:10.7554/eLife.56749
[3] Edwards DN, et al. Selective glutamine metabolism inhibition in tumor cells improves antitumor T lymphocyte activity in triple-negative breast cancer. J Clin Invest. 2021;131(4):e140100. DOI:10.1172/JCI140100 |
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