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Postion:Product Catalog >BAY-8002
BAY-8002
  • BAY-8002

BAY-8002 NEW

Price $33 $76 $113
Package 1mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: BAY-8002 CAS No.: 724440-27-1
Purity: 99.13% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameBAY-8002
DescriptionBAY-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).
Cell ResearchCells 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.
Animal ResearchFor 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.
In vitroBAY-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).
In vivoRaji 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.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 50 mg/mL (120.24 mM)
KeywordsMonocarboxylate Transporter | Inhibitor | inhibit | BAY-8002
Inhibitors Related7ACC1 | AZD0095 | MCT1-IN-3 | Niflumic acid | D-Phenylalanine | AZD3965 | MSC-4381 | α-Cyano-4-hydroxycinnamic acid | 7ACC2 | AR-C155858 | Lactate transportor 1 | VB124
Related Compound LibrariesTarget-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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