V-9302

目录号: GC34852纯度: >99.50%

An inhibitor of ASCT2

Cas No.: 1855871-76-9

规格	价格	库存	数量
1mg	¥324.00	现货	1
5mg	¥810.00	现货	1
10mg	¥1,350.00	现货	1
25mg	¥2,565.00	现货	1
50mg	¥3,582.00	现货	1
100mg	¥5,022.00	现货	1
10mM (in 1mL DMSO)	¥960.00	现货	1

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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

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)

实验参考方法 Experimental Reference Method

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.
References: [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.

产品文档 Product Documents

批次：Purity:>99.50%

化学性质Chemical Properties

CAS 号

1855871-76-9

SMILES

O=C(O)[C@@H](N)CCN(CC1=CC=CC=C1OCC2=CC=CC(C)=C2)CC3=CC=CC=C3OCC4=CC=CC(C)=C4

分子式

C₃₄H₃₈N₂O₄

分子量

538.68 g/mol

溶解性

DMSO : 125 mg/mL (232.05 mM);Water : < 0.1 mg/mL (insoluble)

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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