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BAY-8002

Catalog No. T5208 CAS 724440-27-1

Synonyms: BAY8002, BAY 8002

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).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

BAY-8002, CAS 724440-27-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
5 mg	In stock	$ 76.00
10 mg	In stock	$ 113.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 355.00
100 mg	In stock	$ 578.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 99.34%

Purity: 99.13%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	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).
Targets&IC50	MCT1:85 nM (MCT1-expressing DLD-1 cells)
In vitro	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).
In vivo	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.
Cell Research	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.
Animal Research	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.

Synonyms	BAY8002, BAY 8002
Molecular Weight	415.85
Formula	C20H14ClNO5S
CAS No.	724440-27-1

Storage

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

Solubility Information

DMSO: 50 mg/mL (120.24 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library NO PAINS Compound Library Ion Channel Inhibitor Library Orally Active Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library

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Related compounds with same targets

Niflumic acid α-Cyano-4-hydroxycinnamic acid Lactate transportor 1 AR-C155858 AZD0095 MCT1-IN-3 VB124 7ACC2

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Keywords

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

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.