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生物化工
抑制剂
V-9302
化合物 V-9302
化合物 V-9302|T5345|TargetMol
价格
¥
692
¥
1170
¥
2250
包装
5mg
10mg
25mg
最小起订量
1mg
发货地
上海
更新日期
2025-11-17
QQ交谈
微信洽谈
产品详情
中文名称:
化合物 V-9302
英文名称:
V-9302
CAS:
1855871-76-9
品牌:
TargetMol
产地:
美国
保存条件:
store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
纯度规格:
99.52%
产品类别:
抑制剂
货号:
T5345
2025-11-17
化合物 V-9302
V-9302
5mg/692RMB;10mg/1170RMB;25mg/2250RMB
692
TargetMol
美国
store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
99.52%
抑制剂
Product Introduction
Bioactivity
名称
V-9302
描述
V-9302 (V9302) is a competitive antagonist of transmembrane glutamine flux that selectively and potently targets the amino acid transporter ASCT2 (IC50: 9.6 uM).
细胞实验
Live-cell amino acid uptake assays using HEK293 cells were carried out in 96-well plates. 96-well plates were coated with poly-D-lysine prior to the assay. Cells were plated at a density of 35,000 cells per well 24 h prior to carrying out the assay. Each set of conditions was replicated at least three times, technically and biologically. Cells were washed three times with 100 μL of assay buffer (containing 137 mM NaCl, 5.1 mM KCl, 0.77 mM KH2PO4, 0.71 mM MgSO4.7H2O, 1.1 mM CaCl2, 10 mM D-glucose, and 10 mM HEPES) to remove cell media. 3H-amino acid (500 nM) in the same buffer was added concomitantly with V-9302 and allowed to incubate for 15 min at 37 oC. For ASCT2-mediated 3H-glutamine uptake assays, 5 mM of the system-L inhibitor 2-amino-2-norbornanecarboxylic acid (BCH) was added and the assay buffer was adjusted to pH 6.0. For selectivity studies, no BCH was added and the assay was conducted at pH 7.4. Following the incubation period, the 3H-glutamine/inhibitor was removed and the cells were washed three times with assay buffer. The cells were then lysed by the addition of 50 μL of 1 M NaOH. For reading, 150 μL of scintillation fluid was added and the plates were counted on a scintillation counter. IC50 was calculated using GraphPad Prism.
动物实验
Animal handling methods for PET imaging studies were conducted as reported. Prior to imaging, animals were allowed to acclimate to facility environment for at least 1 h in a warmed chamber at 31.5 °C. Animals were administered 10.4–11.8 MBq 4-[18F]fluoroglutamine via intravenous injection and imaged using a scanner. During imaging, animals were maintained under 2% isoflurane anesthesia in oxygen at 2 L/min and kept warm for the duration of the PET scan. PET images in xenograft-bearing mice were acquired as 60-minute dynamic data sets. Imaging was initiated three hours post-treatment following vehicle or V-9302 (75 mg/kg) administration. PET data were reconstructed using a three-dimensional (3D) ordered subset expectation maximization/maximum a posteriori (OSEM3D/MAP) algorithm. The resulting three-dimensional reconstructions had an x-y voxel size of 0.474 mm and inter-slice distance of 0.796 mm. ASIPro software was used to manually draw 3D regions of interest (ROIs) surrounding the entire tumor volume. 4-[18F]fluoroglutamine uptake was quantified as the percentage of the injected dose per gram of tissue (%ID/g). Significance was calculated using a t-test in Graphpad Prism. Error is reported as standard deviation (SD).
体外活性
V-9302 inhibited ASCT2-mediated glutamine uptake in human cells in a concentration-dependent fashion and exhibited a 100-fold improvement in potency (IC50 V-9302 = 9.6 μM) over gamma-L-glutamyl-p-nitroanilide (GPNA; IC50 = 1000 μM). The EC50 concentrations for the four colorectal cancer (CRC) cell lines exposed to V-9302 ranged from approximately 9-15 μM.
体内活性
Following a single dose of V-9302 (75 mg/kg, 4 h), [18F]-4F-glutamine uptake in tumors was reduced by approximately 50% to levels below background uptake in healthy muscle. Over the treatment course, V-9302 (75 mg/kg/day, 21 days) prevented tumor growth compared to vehicle controls in both HCT-116 and HT29 xenograft models.
存储条件
store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度
H2O : Insoluble
DMSO : 11 mg/mL (20.42 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (18.56 mM), Solution.
关键字
V-9302 | V9302 | V 9302 | uptake | transporter | transmembrane glutamine flux | stress | proliferation | oxidative | nude | mice | Inhibitor | inhibit | HEK-293 | glutamine | flux | athymic
相关产品
GPNA hydrochloride | L-4FPG | Idactamab
相关库
抑制剂库 | 经典已知活性库 | 已知活性化合物库 | NO PAINS 化合物库 | 抗COVID-19化合物库 | 谷氨酰胺代谢化合物库 | 铁死亡化合物库
关键字:
V-9302|TargetMol
公司简介
TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。
成立日期
2013-04-18
(13年)
注册资本
566.265100万人民币
员工人数
100-500人
年营业额
¥ 1亿以上
主营行业
天然产物,生化试剂,分子生物学,分子砌块,生物技术服务
经营模式
贸易,工厂,试剂,定制,服务
TargetMol中国(陶术生物)
VIP
4年
公司成立:
13年
注册资本:
566.265100万人民币
企业类型:
有限责任公司(自然人投资或控股)
主营产品:
小分子抑制剂、药物筛选化合物库、药物筛选等
公司地址:
静安区江场三路238号8楼
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