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CAS No. : 1855871-76-9
MCE 国际站:V-9302
产品活性: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)。
In Vitro: 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.
In Vivo: 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.
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