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).

MCT1:85 nM (MCT1-expressing DLD-1 cells)

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）。

Raji肿瘤小鼠每日两次通过口服方式接受了80与160 mg/kg BAY-8002治疗。BAY-8002在抑制肿瘤生长方面显示出显著效果，但未观察到肿瘤退缩。Daudi Burkitt's淋巴瘤模型对MCT1抑制有所响应，尽管对于BAY-8002来说并不显著。

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.

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.