| Identification | Back Directory | [Name]
V-9302 | [CAS]
1855871-76-9 | [Synonyms]
V-9302
V-9302 HCL
V-9302; V9302; V 9302
Butanoic acid, 2-amino-4-[bis[[2-[(3-methylphenyl)methoxy]phenyl]methyl]amino]-, (2S)- | [Molecular Formula]
C34H38N2O4 | [MDL Number]
MFCD32062750 | [MOL File]
1855871-76-9.mol | [Molecular Weight]
538.68 |
| Chemical Properties | Back Directory | [Boiling point ]
688.7±55.0 °C(Predicted) | [density ]
1.179±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:85.0(Max Conc. mg/mL);157.79(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.61(Max Conc. mM)
DMF:25.0(Max Conc. mg/mL);46.41(Max Conc. mM)
Ethanol:60.0(Max Conc. mg/mL);111.38(Max Conc. mM)
Water:50.5(Max Conc. mg/mL);93.75(Max Conc. mM) | [form ]
A crystalline solid | [pka]
2.08±0.10(Predicted) | [color ]
White to yellow | [InChIKey]
YGKNVAAMULVFNN-HKBQPEDESA-N | [SMILES]
CC1=CC=CC(COC2=C(C=CC=C2)CN(CC3=CC=CC=C3OCC4=CC=CC(C)=C4)CC[C@@H](C(O)=O)N)=C1 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
V-9302 is a selective competitive antagonist of the amino acid transporter ASCT2 (SLC1A5) with anti-tumor activity. V-9302 caused reduced cellular viability and increased cell death in a panel of cancer cell lines and reduced tumor cell growth in both HCT-116 and HT29 (Fig. 5f) xenograft models. | [in vivo]
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]. | Animal Model: | 6-week old, female athymic nude mice (bearing HCT-116 (KRAS G13D) or HT29 (BRAF V600E) cell-line)[1] | | Dosage: | 75 mg/kg | | Administration: | Intraperitoneally; daily fo 21 days | | Result: | Prevented tumor growth.
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| [IC 50]
ASCT2 | [References]
[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. DOI:10.1038/nm.4464
[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. DOI:10.7554/eLife.56749
[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. DOI:10.1172/JCI140100 |
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| Company Name: |
BOC Sciences
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| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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