BAY-8002 |
Catalog No.GC19488
One-Click Copy Product Info
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BAY-8002 est un inhibiteur puissant, sélectif et actif par voie orale du transporteur de monocarboxylate 1 (MCT1), avec une IC50 de 85 nM dans les cellules DLD-1 exprimant MCT1, affiche une excellente sélectivité contre MCT4. Activité anti-tumorale.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 724440-27-1
Sample solution is provided at 25 µL, 10mM.
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BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85nM[1]. BAY-8002 targets MCT1 to regulate the MCT1-mTOR signaling pathway, thereby increasing autophagy and influencing the formation of mineralized nodules and the expression of osteogenic-related proteins[2]. BAY-8002 has been widely used to regulate the expression of SLC16A1 to alter the response of prostate cancer cells to afatinib[3].
In vitro, BAY-8002 treatment (10µM) for 5 days significantly inhibited lipid accumulation in immortalized mouse E12.5 hepatic progenitor (iHPx) cells, and reduced the expression of genes involved in the synthesis and regulation of triglycerides and fatty acids[4]. Treatment with 1µM BAY-8002 for 1 hour increased the nuclear translocation of the DNA-PK catalytic subunit (DNA-PKcs), enhanced lactate flux, and decreased the transduction efficiency of lentivirus in HeLa cells[5]. 100nM of BAY-8002 incubated for 24 hours, which restrained the migration of MCF-7 cells stimulated by matrix cell-conditioned medium (CM)[6]. 75µM of BAY-8002 pretreatment for 1 hour reduced the extracellular lactate level and inhibited the expression of IL-9 in human T helper 9 (TH9) cells[7].
In vivo, BAY-8002 treatment via oral administration at a dose of 160mg/kg twice daily for 28 days significantly suppressed tumor growth in Raji Burkitt lymphoma tumor-bearing mice, without affecting the body weight[1].
References:[1] Quanz M, Bender E, Kopitz C, et al. Preclinical efficacy of the novel monocarboxylate transporter 1 inhibitor BAY-8002 and associated markers of resistance[J]. Molecular Cancer Therapeutics, 2018, 17(11): 2285-2296.
[2] Luo Y, Gou H, Chen X, et al. Lactate inhibits osteogenic differentiation of human periodontal ligament stem cells via autophagy through the MCT1-mTOR signaling pathway[J]. Bone, 2022, 162: 116444.
[3] Matheux A, Gassiot M, Fromont G, et al. PXR modulates the prostate cancer cell response to afatinib by regulating the expression of the monocarboxylate transporter SLC16A1[J]. Cancers, 2021, 13(14): 3635.
[4] Gou Y, Li A, Dong X, et al. Lactate transporter MCT4 regulates the hub genes for lipid metabolism and inflammation to attenuate intracellular lipid accumulation in non-alcoholic fatty liver disease[J]. Genes & Diseases, 2025, 12(4): 101554.
[5] Wagner W, Sobierajska K, Kania K D, et al. Lactate suppresses retroviral transduction in cervical epithelial cells through DNA-PKcs modulation[J]. International Journal of Molecular Sciences, 2021, 22(24): 13194.
[6] Vera M J, Ponce I, Almarza C, et al. CCL2 and lactate from chemotherapeutics-treated fibroblasts drive malignant traits by metabolic rewiring in low-migrating breast cancer cell lines[J]. Antioxidants, 2024, 13(7): 801.
[7] Bertschi N L, Steck O, Luther F, et al. PPAR-γ regulates the effector function of human T helper 9 cells by promoting glycolysis[J]. Nature Communications, 2023, 14(1): 2471.
| Cell experiment [1]: | |
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Cell lines |
Immortalized mouse E12.5 hepatic progenitor (iHPx) cells |
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Preparation Method |
The iHPx cells were cultured in DMEM medium, supplemented with 10% fetal bovine serum, 100U/ml penicillin, and 100μg/ml of streptomycin at 37°C in an incubator with 5% CO2. Subconfluent iHPx cells were seeded in 96-well plates (4000 cells/well) and treated with different concentrations of BAY-8002 (0, 1, 10, and 100µM). After 72h, cell viability was tested. |
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Reaction Conditions |
0, 1, 10, and 100µM; 48h |
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Applications |
BAY-8002 treatment markedly reduced viability of iHPx cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Female NOD SCID mice |
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Preparation Method |
Female NOD SCID mice (7 weeks old) were housed in SPF conditions with an automatic 12h/12h light-dark cycle at a constant temperature (20-25°C). Raji cells were s.c. injected in 0.1ml suspension to the left flank of mice (3×106 cells in 10% matrigel). Tumor area (length×width) and body weight were determined at least twice weekly. Raji tumor-bearing mice were treated with 160mg/kg BAY-8002 twice daily, and tumors were collected for analysis after 28 days. |
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Dosage form |
160mg/kg; twice a day; 28 days; p.o. |
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Applications |
BAY-8002 treatment suppressed tumor growth in Raji tumor-bearing mice, without affecting body weight. |
| References: [1] Gou Y, Li A, Dong X, et al. Lactate transporter MCT4 regulates the hub genes for lipid metabolism and inflammation to attenuate intracellular lipid accumulation in non-alcoholic fatty liver disease[J]. Genes & Diseases, 2025, 12(4): 101554. [2] Quanz M, Bender E, Kopitz C, et al. Preclinical efficacy of the novel monocarboxylate transporter 1 inhibitor BAY-8002 and associated markers of resistance[J]. Molecular Cancer Therapeutics, 2018, 17(11): 2285-2296. | |
| Cas No. | 724440-27-1 | SDF | |
| Canonical SMILES | O=C(O)C1=CC=CC=C1NC(C2=CC(S(=O)(C3=CC=CC=C3)=O)=CC=C2Cl)=O | ||
| Formula | C₂₀H₁₄ClNO₅S | M.Wt | 415.85 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4047 mL | 12.0236 mL | 24.0471 mL |
| 5 mM | 480.9 μL | 2.4047 mL | 4.8094 mL |
| 10 mM | 240.5 μL | 1.2024 mL | 2.4047 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)