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V-9302 hydrochloride is a competitive transmembrane glutamine flux antagonist that selectively targets the amino acid transporter ASCT2/SLC1A5. V-9302 hydrochloride impedes glutamine uptake mediated by ASCT2 (IC50=9.6 μM), inhibits the mTOR signalling pathway, increases oxidative stress and ROS levels, induces autophagy, and exerts antitumour effects.


| Description | V-9302 hydrochloride is a competitive transmembrane glutamine flux antagonist that selectively targets the amino acid transporter ASCT2/SLC1A5. V-9302 hydrochloride impedes glutamine uptake mediated by ASCT2 (IC50=9.6 μM), inhibits the mTOR signalling pathway, increases oxidative stress and ROS levels, induces autophagy, and exerts antitumour effects. |
| In vitro | V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake in Homo sapiens cells in a concentration-dependent manner, with a potency 100 times higher than γ-L-glutamyl-p-nitroaniline [1]. Pharmacological blockade of ASCT2 by V-9302 hydrochloride reduces cancer cell growth and proliferation, increases cell mortality, and intensifies oxidative stress [1]. |
| In vivo | V-9302 hydrochloride (75 mg/kg, once daily for 21 days) administered intraperitoneally to HCT-116 and HT29 parazacco spilurus subsp. spilurus xenograft mouse models effectively prevents tumor growth [1]. V-9302 hydrochloride (30 mg/kg, once daily, 5 days/week) administered intraperitoneally to SNU398 and MHCC97H parazacco spilurus subsp. spilurus xenograft models, when combined with CB-839, induces significant tumor growth inhibition, while monotherapy shows moderate antitumor effects [2]. V-9302 hydrochloride (50 mg/kg, once daily for 5 days) administered intraperitoneally to a mouse triple-negative breast cancer (TNBC) orthotopic tumor model significantly reduces tumor growth [3]. |
| Synonyms | V9302 hydrochloride |
| Molecular Weight | 575.14 |
| Formula | C34H39ClN2O4 |
| Cas No. | 2416138-42-4 |
| Smiles | C(N(CC1=C(OCC2=CC(C)=CC=C2)C=CC=C1)CC[C@@H](C(O)=O)N)C3=C(OCC4=CC(C)=CC=C4)C=CC=C3.Cl |
| Color | Yellow |
| Appearance | Solid |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 40 mg/mL (69.55 mM) DMSO: 80 mg/mL (139.1 mM) | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.74 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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