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AZD3965

AZD3965

产品编号 T3210   CAS 1448671-31-5
别名: AZD 3965, AZD-3965

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。

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AZD3965 Chemical Structure
AZD3965, CAS 1448671-31-5
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
产品目录号及名称: AZD3965 (T3210)
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选择批次  
纯度: 99.85%
纯度: 99.75%
纯度: 99.71%
纯度: 99.35%
纯度: 98.99%
纯度: 98.03%
纯度: 98%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 100 mg/mL (193.98 mM)

DMSO: 100 mg/mL (193.98 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Critchlow SE, et al. 2012. AACR 103rd Annual Meeting. 2. Polański R, et al. Clin Cancer Res. 2014, 20(4), 926-937. 3. Bola BM, et al. Mol Cancer Ther. 2014, 13(12), 2805-2816.

文献引用

1. Li F F, Zhang Y L, Guo D X, et al. Biochemometric approach combined with 1D CSSF-TOCSY for the identification of sensitization agents in Curcuma longa L. and prediction of their action mechanisms. Microchemical Journal. 2022 October 2. Li X, Zhang Y, Xu L, et al.Ultrasensitive sensors reveal the spatiotemporal landscape of lactate metabolism in physiology and disease.Cell Metabolism.2023, 35(1): 200-211. e9. 3. Zhang Y T, Xing M L, Fang H H, et al.Effects of lactate on metabolism and differentiation of CD4+T cells.Molecular Immunology.2023, 154: 96-107.
7ACC1 Niflumic acid α-Cyano-4-hydroxycinnamic acid Lactate transportor 1 AR-C155858 AZD0095 BAY-8002 7ACC2

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌临床化合物库 抗癌药物库 药物功能重定位化合物库 离子通道库 抑制剂库 表型筛选靶点鉴定库 临床前化合物库 ReFRAME 相关化合物库 已知活性化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

AZD3965 1448671-31-5 Membrane transporter/Ion channel Monocarboxylate transporter inhibit Inhibitor Monocarboxylate Transporter AZD 3965 AZD-3965 inhibitor

 

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