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BAY-8002

BAY-8002

产品编号 T5208   CAS 724440-27-1
别名: BAY8002, BAY 8002

BAY-8002 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。

TargetMol的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。
BAY-8002 Chemical Structure
BAY-8002, CAS 724440-27-1
规格 价格/CNY 货期 数量
1 mg ¥ 278 现货
5 mg ¥ 655 现货
10 mg ¥ 987 现货
25 mg ¥ 1,980 现货
50 mg ¥ 2,950 现货
100 mg ¥ 4,350 现货
1 mL * 10 mM (in DMSO) ¥ 719 现货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: BAY-8002 (T5208)
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纯度: 99.34%
纯度: 99.13%
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生物活性
化学信息
存储 & 溶解度
参考文献
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).
靶点活性 MCT1:85 nM (MCT1-expressing DLD-1 cells)
体外活性 在DLD-1细胞中表达MCT1的情况下,BAY-8002以85 nM的IC50值抑制了细胞内SNARF-5的荧光变化,并且在抑制MCT4时表现出极佳的选择性(在EVSA-T细胞中的IC50>50 μmol/L)。
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.
别名 BAY8002, BAY 8002
分子量 415.85
分子式 C20H14ClNO5S
CAS No. 724440-27-1

存储

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

溶解度

DMSO: 50 mg/mL (120.24 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4047 mL 12.0236 mL 24.0471 mL 60.1178 mL
5 mM 0.4809 mL 2.4047 mL 4.8094 mL 12.0236 mL
10 mM 0.2405 mL 1.2024 mL 2.4047 mL 6.0118 mL
20 mM 0.1202 mL 0.6012 mL 1.2024 mL 3.0059 mL
50 mM 0.0481 mL 0.2405 mL 0.4809 mL 1.2024 mL
100 mM 0.024 mL 0.1202 mL 0.2405 mL 0.6012 mL

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TargetMol Library Books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.
7ACC1 Niflumic acid α-Cyano-4-hydroxycinnamic acid Lactate transportor 1 AR-C155858 AZD0095 MCT1-IN-3 7ACC2

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 膜蛋白靶向化合物库 抗癌活性化合物库 抗癌化合物库 表型筛选靶点鉴定库 经典已知活性库 NO PAINS 化合物库 口服活性化合物库 离子通道库 已知活性化合物库

TargetMol Calculator剂量换算

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TargetMol Calculator 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
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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。
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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

BAY-8002 724440-27-1 Membrane transporter/Ion channel Monocarboxylate transporter Monocarboxylate Transporter BAY8002 Inhibitor inhibit BAY 8002 inhibitor

 

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