V9302

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

V-9302 (V9302) 是一种跨膜谷氨酰胺通量的竞争性拮抗剂，选择性有效地靶向氨基酸转运蛋白 ASCT2 (IC50: 9.6 uM)。

V-9302 (V9302) is a competitive antagonist of transmembrane glutamine flux that selectively and potently targets the amino acid transporter ASCT2 (IC50: 9.6 uM).

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.

V-9302 (75 mg/kg; i.p.; daily fo 21 days) prevents tumor growth in both HCT-116 and HT29 xenograft models.The combination ofCB-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. Animal Model:6-week old, female athymic nude mice (bearing HCT-116 (KRAS G13D) or HT29 (BRAF V600E) cell-line)Dosage:75 mg/kg Administration:Intraperitoneally; daily fo 21 daysResult:Prevented tumor growth.

V 9302 | V-9302

Others

Other Targets

ASCT2

——

——

1855871-76-9

538.69

C34H38N2O4

>98% (HPLC)

DMSO: 100 mg/mL (185.64 mM);Water: Insoluble

Cc1cccc(COc2ccccc2CN(CC[C@H](N)C(O)=O)Cc2ccccc2OCc2cccc(C)c2)c1

(S)-2-Amino-4-(bis(2-((3-methylbenzyl)oxy)benzyl)amino)butanoic acid

(-20℃)

With Ice Pack

≥ 2 years