Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD3965 (AZD-3965) 是单羧酸转运蛋白 1 (MCT1) 的选择性抑制剂,Ki 值为1.6 nM,比 MCT2的选择性高6倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 798 | 现货 | ||
5 mg | ¥ 1,237 | 现货 | ||
10 mg | ¥ 1,998 | 现货 | ||
25 mg | ¥ 3,598 | 现货 | ||
50 mg | ¥ 4,870 | 现货 | ||
100 mg | ¥ 6,950 | 现货 | ||
200 mg | ¥ 9,380 | 现货 | ||
500 mg | ¥ 14,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,410 | 现货 |
产品描述 | AZD3965 (AZD-3965) is a selective inhibitor of monocarboxylate transporter 1 (MCT1). |
靶点活性 | MCT1:1.6 nM (Ki) |
体外活性 | In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth. [1] AZD3965 inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia. [2] In H526, HGC27 cells and DMS114 cells, AZD3965 increases intracellular lactate and significantly reduces lactate uptake. [3] |
体内活性 | In nonobese diabetic scid-γ mice bearing COR-L103 xenografts, AZD3965 (100 mg/kg, p.o.) reduces tumor growth and increased intratumor lactate. [2] In mice bearing H526 tumors, AZD3965 (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity. [3] |
激酶实验 | Cells are plated overnight and treated with 100 nM AZD3965 or vehicle for 24 hours. The cells are then washed, once in PBS and twice with lysis buffer (50 mM Mops, 100 mM KCl, 5 mM MgCl2, 1 mM EDTA, 0.1 mM DTT, 1 mM PMSF supplemented with 1× mini complete protease inhibitor cocktail tablets. The cells are harvested by scraping and centrifugation, and the pellet snap frozen without buffer in liquid nitrogen. Frozen aliquots of cells are thawed on ice and re-suspended in lysis buffer. Cells are lysed by 3 rounds of freezing in liquid nitrogen and thawing at 37°C for 2 minutes each. Lysates are subsequently centrifuged (13000 g, 10min, 4°C) until clear and then stored on ice. Enzyme activity in the cell lysates is determined using a micro-plate reader to measure either production or depletion of NADH/NADPH, through its absorbance at 340/10 nm, occurring as a result of direct or coupled enzyme reactions. The 96 well plates used for the assays are pre-heated to 37°C for 10 minutes prior to starting reactions, initiated by the addition of 5 μL cell lysate to 95 μL of reaction buffer (50 mM Mops pH 7.4, 100 mM KCl, 5 mM free magnesium). The standard reaction buffer is supplemented to assay the kinetics of the different enzymes. Absorbance values for controls are subtracted from absorbance of corresponding reactions. Graphpad prism 6 is used to plot V0 values against substrate concentration and determine Vmax and Km values. The Vmax is then normalised to the protein concentration in the cell lysate[1]. |
别名 | AZD 3965, AZD-3965 |
分子量 | 515.51 |
分子式 | C21H24F3N5O5S |
CAS No. | 1448671-31-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 100 mg/mL (193.98 mM)
DMSO: 100 mg/mL (193.98 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.9398 mL | 9.6991 mL | 19.3983 mL | 48.4957 mL |
5 mM | 0.388 mL | 1.9398 mL | 3.8797 mL | 9.6991 mL | |
10 mM | 0.194 mL | 0.9699 mL | 1.9398 mL | 4.8496 mL | |
20 mM | 0.097 mL | 0.485 mL | 0.9699 mL | 2.4248 mL | |
50 mM | 0.0388 mL | 0.194 mL | 0.388 mL | 0.9699 mL | |
100 mM | 0.0194 mL | 0.097 mL | 0.194 mL | 0.485 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。
AZD3965 1448671-31-5 Membrane transporter/Ion channel Monocarboxylate transporter inhibit Inhibitor Monocarboxylate Transporter AZD 3965 AZD-3965 inhibitor