V-9302

An inhibitor of ASCT2

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
5mg

￥987.00

790.00

- +
10mg

￥1625.00

1300.00

- +
25mg

￥3100.00

2480.00

- +
50mg

￥5500.00

4400.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajce53946
CAS: 1855871-76-9
别名:
分子式: C34H38N2O4
分子量: 538.68
纯度: >98%
溶解度: DMSO : 125 mg/mL (232.05 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

V-9302 is an inhibitor of amino acid transporter 2 (ASCT2).¹ It inhibits glutamine uptake with IC₅₀ values of 9 and 9.6 ?M for the rat and human transporters, respectively. V-9302 also inhibits glutamine uptake in HEK293 cells and reduces cell viability of a variety of cancer cell lines, including HCT116, HT-29, COLO 205, and RKO cells (EC₅₀s = 8.9, 9.4, 14.5, and 8.3 ?M, respectively).² It reduces glutamine uptake into tumor tissue and prevents tumor growth in HCT116 and HT-29 mouse xenograft models expressing K-Ras^G13D and BRAF^V600E mutations, respectively, when administered at a dose of 75 mg/kg per day for 21 days.

1.Schulte, M.L., Khodadadi, A.B., Cuthbertson, M.L., et al.2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transportBioorg. Med. Chem. Lett.26(3)1044-1047(2016) 2.Schulte, M.L., Fu, A., Zhao, P., et al.Pharmacological blockade of ASCT2-dependent glutamine transport leads to antitumor efficacy in preclinical modelsNat. Med.24(2)194-202(2018)

Protocol

Cell experiment [1]:
Cell lines	HCC1806 cells
Preparation Method	Cells were plated in 96-well plates for 24 h before the assay. Cells were treated with either vehicle or the indicated concentrations（25 μM） of V-9302 hydrochloride for 48 h
Reaction Conditions	25 μM，48h
Applications	Silencing of ASCT2 and V-9302 hydrochloride exposure in HCC1806 cells resulted in analogous downstream effects, including markedly decreased phosphorylated (p)-S6 levels and a modest decrease in p-ERK levels.
Animal experiment [2]:
Animal models	6-week-old female athymic nude mice
Preparation Method	Chronic-exposure studies in tumor-bearing mice. Athymic nude mice (Hsd:Athymic nude-Foxn1nu) bearing HCT-116 (KRAS-G13D) or HT29 (BRAF-V600E) cell line xenografts were treated with 75 mg V-9302 hydrochloride per kg body weight per day for 21 d.
Dosage form	75 mg V-9302 hydrochloride per kg body weight per day for 21 day
Applications	V-9302 hydrochloride led to significantly decreased expression of p-S6 in tumor tissue in both HCT-116 and HT29 xenografts. In addition to decreased p-S6 IHC staining, V-9302 treatment led to elevated levels of cleaved caspase 3 in both HCT-116 and HT29 xenografts.
参考文献: [1]. Schulte ML, Fu A, et,al. Pharmacological blockade of ASCT2-dependent glutamine transport leads to antitumor efficacy in preclinical models. Nat Med. 2018 Feb;24(2):194-202. doi: 10.1038/nm.4464. Epub 2018 Jan 15. PMID: 29334372; PMCID: PMC5803339.