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化合物 V-9302,V-9302

化合物 V-9302|T5345|TargetMol

價格 479 728 1237
包裝 2mg 5mg 10mg
最小起訂量 1mg
發(fā)貨地 上海
更新日期 2024-12-12
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產(chǎn)品詳情

中文名稱:化合物 V-9302英文名稱:V-9302
CAS:1855871-76-9品牌: TargetMol
產(chǎn)地: 美國保存條件: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
純度規(guī)格: 99.67%產(chǎn)品類別: 抑制劑
貨號: T5345
2024-12-12 化合物 V-9302 V-9302 2mg/479RMB;5mg/728RMB;10mg/1237RMB 479 TargetMol 美國 store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.67% 抑制劑

Product Introduction

Bioactivity

名稱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).
細胞實驗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.
動物實驗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).
體外活性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.
體內(nèi)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.
存儲條件store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : Insoluble
DMSO : 6.25 mg/mL (11.6 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (18.56 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
關鍵字proliferation | V-9302 | stress | mice | flux | V9302 | uptake | transporter | athymic | Inhibitor | glutamine | nude | inhibit | oxidative | HEK-293 | V 9302
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關鍵字: V-9302|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓,致力于為全球生化領域科學家的研究提供專業(yè)的產(chǎn)品和服務。TargetMol?品牌的客戶群分布于40多個國家和地區(qū),已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應商。 TargetMol?可提供160多種滿足不同需求的化合物庫,以及多種類型的生化試劑產(chǎn)品,包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學試劑盒等,此外,我們還建設有CADD(計算機輔助藥物設計)研究中心、藥理實驗室、藥化合成平臺三大技術中心,全方位滿足客戶的定制需求。 憑借我們優(yōu)質(zhì)的產(chǎn)品和服務、快速高效的全球供應鏈和專業(yè)的技術支持,我們將有效幫助您縮短研發(fā)周期,取得更成功的結果。
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