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1855871-76-9-V-9302 V-9302

V-9302

For research use only. Not for therapeutic Use.

  • CAT Number: I019215
  • CAS Number: 1855871-76-9
  • Molecular Formula: C34H38N2O4
  • Molecular Weight: 538.68
  • Purity: ≥95%
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Related Small Molecules: CRAC intermediate 2     {Boc}-Phe-Leu-Phe-Leu-Phe     Cimiracemoside C    

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 (IC50=9.6 µM) in HEK-293 cells[1].
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[1].
Pharmacological blockade of ASCT2 with V-9302 results in attenuated cancer cell growth and proliferation, increases cell death, and increases oxidative stress[1].
V-9302 (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].


Catalog Number I019215
CAS Number 1855871-76-9
Synonyms

(2S)-2-amino-4-[bis[[2-[(3-methylphenyl)methoxy]phenyl]methyl]amino]butanoic acid

Molecular Formula C34H38N2O4
Purity ≥95%
InChI InChI=1S/C34H38N2O4/c1-25-9-7-11-27(19-25)23-39-32-15-5-3-13-29(32)21-36(18-17-31(35)34(37)38)22-30-14-4-6-16-33(30)40-24-28-12-8-10-26(2)20-28/h3-16,19-20,31H,17-18,21-24,35H2,1-2H3,(H,37,38)/t31-/m0/s1
InChIKey YGKNVAAMULVFNN-HKBQPEDESA-N
SMILES CC1=CC(=CC=C1)COC2=CC=CC=C2CN(CCC(C(=O)O)N)CC3=CC=CC=C3OCC4=CC=CC(=C4)C
Reference

[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]

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