V-9302
V-9302 Basic information
- Product Name:
- V-9302
- Synonyms:
-
- V-9302 HCL
- V-9302
- V-9302; V9302; V 9302
- Butanoic acid, 2-amino-4-[bis[[2-[(3-methylphenyl)methoxy]phenyl]methyl]amino]-, (2S)-
- V-9302 1855871-76-9
- proliferation,stress,mice,flux,uptake,transporter,athymic,Inhibitor,V 9302,V9302,glutamine,nude,inhibit,V-9302,oxidative,HEK-293
- (S)-2-Amino-4-(bis(2-((3-methylbenzyl)oxy)benzyl)amino)butanoic acid
- V-9302 ，S8818
- CAS:
- 1855871-76-9
- MF:
- C34H38N2O4
- MW:
- 538.68
- Mol File:
- 1855871-76-9.mol
V-9302 Chemical Properties
- 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
V-9302 Usage And Synthesis
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. |
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
V-9302Supplier
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Tel
- 021-54135696 18516235431
- shgegenetech@163.com
- Tel
- 027-87465837 19945049750
- sales@finetechnology-ind.com
- Tel
- 15221275939
- shenlinxing@macklin.cn
- Tel
- 021-52996696，15000506266 15000506266