ChemicalBook CAS DataBase List 2416138-42-4

2416138-42-4

Name	V-9302 HCl
CAS	2416138-42-4
Molecular Formula	C34H39ClN2O4
Molecular Weight	575.15
MOL File	2416138-42-4.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMSO: 250 mg/mL (434.68 mM)
form	Solid
color	White to off-white

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P305+P351+P338

Hazard Information

Uses

V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 μM) in HEK-293 cells[1].

in vivo

V-9302 hydrochloride (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 (KRASG13D) or HT29 (BRAFV600E) 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

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