V-9302 是跨膜谷氨酰胺通量的竞争性拮抗剂。V-9302 有效选择性的靶向氨基酸转运体 ASCT2 (SLC1A5)，不是 ASCT1。V-9302 抑制了 HEK-293 细胞中由 ASCT2 介导的谷氨酰胺摄取 (IC₅₀=9.6 μM)。

V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC 50 =9.6 μM) in HEK-293 cells.

Solid

ASCT2

V-9302 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.
Pharmacological blockade of ASCT2 with V-9302 results in attenuated cancer cell growth and proliferation, increases cell death, and increases oxidative stress. has not independently confirmed the accuracy of these methods. They are for reference only.

V-9302 (75 mg/kg; i.p.; daily fo 21 days) prevents tumor growth in both HCT-116 and HT29 xenograft models.
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.
V-9302 (50 mg/kg ; i.p.; daily for 5 days) displays markedly reduced tumor growth. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.
[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.

In Vitro: DMSO : 25 mg/mL (46.41 mM; ultrasonic and warming and heat to 80°C)H₂O : < 0.1 mg/mL (ultrasonic) (insoluble)配制储备液