V-9302 hydrochlorideV-9302 hydrochloride
MedChemExpress (MCE)
HY-112683A
2416138-42-4
99.34%
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
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.
V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake in human cells in a concentration-dependent fashion and exhibits a 100-fold improvement in potency over gamma-L-glutamyl-p-nitroanilide[1]. Pharmacological blockade of ASCT2 with V-9302 hydrochloride results in attenuated cancer cell growth and proliferation, increases cell death, and increases oxidative stress[1].
V-9302 hydrochloride (75 mg/kg
i.p.
daily fo 21 days) prevents tumor growth in both HCT-116 and HT29 xenograft models[1]. 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]. V-9302 (50 mg/kg
i.p.
daily for 5 days) displays markedly reduced tumor growth[3].
ASCT2
| | | |
| | | | | |
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]