BAY-8002

产品编号: T5208 别名:

BAY8002,BAY 8002

BAY8002 是一种可口服的单羧酸转运蛋白第 1 亚型 MCT1 选择性抑制剂，在表达 MCT1 的 DLD-1 细胞中，IC50值为 85 nM，具有抗肿瘤活性。

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CAS：724440-27-1

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

BAY-8002 is a potent dual MCT1/2 inhibitor (IC50 values are 3, 8, and 12 nM at rat (C6), human (DLD-1) and mouse (4T1) MCT1 respectively).

体外活性

BAY-8002 inhibited cellular SNARF-5 fluorescence change with an IC50 of 85 nM in MCT1-expressing DLD-1 cells and displayed excellent selectivity against MCT4 (IC50 >50 μmol/L in EVSA-T cells).

体内活性

Raji tumor-bearing mice were treated twice daily per os with 80 and 160 mg/kg BAY-8002. BAY-8002 showed significant inhibition of tumor growth, however, no tumor regression was observed. Daudi Burkitt's lymphoma model showed some response to MCT1 inhibition, albeit not significant for BAY-8002.

细胞实验

Cells were seeded at 3000- 6000 cells per well in a 90 μl volume in 96-well plates. Triplicates were treated in a dose range of 0-10 μmol/L. Cells were continuously exposed to the drug at 37°C and 5 % CO2. After 72 h, cell viability was measured using the CellTiter Glo cell viability assay. For the generation of resistant cell lines, cells were treated at IC50 and upon regrowth treated with increasing concentrations of the drug.

动物实验

For in vivo studies, tumor cells were subcutaneously (s.c.) injected in 0.1 ml suspension to the left flank of 7-10 weeks old immunocompromised female mice (3 x 10^6 Raji cells in 10% Matrigel) to NOD SCID mice, 2 x 10^6 Colo320DM cells in 50% MatrigelTM to NMRI nu/nu mice, 3 x 10^6 WSU-DLCL2 cells or 1 x 10^7 Daudi cells in 50% MatrigelTM to CB17 SCID mice. Tumor area (length x width) and body weight was determined at least twice weekly. Tumors were allowed to establish before mice were allocated to different treatment and control groups by stratified randomization based on their primary tumor size. Oral treatments (p.o.) via gavage were performed as indicated. Final tumor weights were determined at the end of each study. For statistical analysis of tumor area as well as final tumor weights, data were analyzed using one-way ANOVA followed by Tukey's multiple comparisons test.

Cas No.

724440-27-1

分子式

C20H14ClNO5S

分子量

415.84

别名

BAY8002;BAY 8002;BAY-8002

参考文献

[1]Quanz M, et al. Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance. Mol Cancer Ther. 2018 Nov;17(11):2285-2296.

储存和溶解度

DMSO:50 mg/mL (120.24 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 BAY-8002 724440-27-1

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

体内实验配液计算器

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 ul

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

% DMSO +

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计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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体积

分子量

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制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

浓度（起始）

体积（起始）

浓度（终点）

体积（终点）

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技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

Monocarboxylate Transporter Inhibitor BAY8002 BAY-8002 inhibit BAY 8002 724440-27-1

BAY-8002 相关推荐

相关化合物库推荐该产品包含在如下化合物库中：

注册成功

BAY-8002

BAY8002,BAY 8002

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