store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
V-9302 是一种跨膜谷氨酰胺通量的竞争性拮抗剂。它选择性的靶向氨基酸转运体 ASCT2 (SLC1A5),不影响 ASCT1。它能够阻碍 HEK-293 细胞中由 ASCT2 介导的谷氨酰胺摄取 (IC50=9.6 μM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 479 | 现货 | ||
5 mg | ¥ 728 | 现货 | ||
10 mg | ¥ 1,237 | 现货 | ||
25 mg | ¥ 2,377 | 现货 | ||
50 mg | ¥ 2,990 | 现货 | ||
100 mg | ¥ 4,470 | 现货 | ||
200 mg | ¥ 6,370 | 现货 |
产品描述 | 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). |
靶点活性 | ASCT2:9.6 μM (in HEK-293 cells) |
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. |
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). |
分子量 | 538.68 |
分子式 | C34H38N2O4 |
CAS No. | 1855871-76-9 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 100 mg/mL (185.64 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8564 mL | 9.2819 mL | 18.5639 mL | 46.4097 mL |
5 mM | 0.3713 mL | 1.8564 mL | 3.7128 mL | 9.2819 mL | |
10 mM | 0.1856 mL | 0.9282 mL | 1.8564 mL | 4.641 mL | |
20 mM | 0.0928 mL | 0.4641 mL | 0.9282 mL | 2.3205 mL | |
50 mM | 0.0371 mL | 0.1856 mL | 0.3713 mL | 0.9282 mL | |
100 mM | 0.0186 mL | 0.0928 mL | 0.1856 mL | 0.4641 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
V-9302 1855871-76-9 Others proliferation stress mice flux V9302 uptake transporter athymic Inhibitor glutamine nude inhibit oxidative HEK-293 V 9302 inhibitor