BAY-876 |
Catalog No.GC19061
One-Click Copy Product Info
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BAY-876 is a selective glucose transporter 1 (GLUT1) inhibitor with IC50 of 2 nM. The IC50 of BAY-876 for GLUT2, GLUT3 and GLUT4 are 10.8, 1.67 and 0.29μM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1799753-84-6
Sample solution is provided at 25 µL, 10mM.
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BAY-876 is a selective glucose transporter 1 (GLUT1) inhibitor with IC50 of 2 nM[1]. The IC50 of BAY-876 for GLUT2, GLUT3 and GLUT4 are 10.8, 1.67 and 0.29μM, respectively[1]. BAY-876 blocks glucose transport into tumor cells by inhibiting GLUT activity, thereby effectively inhibiting glucose uptake and tumor cell growth [2].
In vitro, BAY-876 (75nM) treated SKOV-3, OVCAR-3, HEY and A2780 cells for 72h and had a growth inhibitory effect on SKOV-3, OVCAR-3 and HEY cells, but not on A2780 cells [3] . BAY-876 (10 nM, 25 nM, 50 nM) treated CD4+ T cells and macrophages for 24 hours, significantly weakening the glucose uptake of cells and reducing the levels of inflammatory factors [4]. BAY-876 (10-1000µM) treated the renal adenocarcinoma 786-O cell line for 96 hours and significantly inhibited cell proliferation, with an IC50 of 53.56µM [5].
In vivo, BAY-876 (0, 1.5, 3.0, and 4.5 mg/kg/day) dose-dependently reduced tumor volume in NSG mice harboring SKOV-3 xenografts administered orally for 4 weeks and was effective in mice. Body weight has no effect [3]. BAY-876 (5 mg/kg/day) was administered orally for 2 days to mice bearing MHCC 97-H xenografts, which significantly inhibited tumor tissue formation and glucose uptake by cells in the tissue [6].
References:
[1] Siebeneicher H, Cleve A, Rehwinkel H, et al. Identification and optimization of the first highly selective GLUT1 inhibitor BAY‐876[J]. ChemMedChem, 2016, 11(20): 2261-2271.
[2] Kopitz C, Toschi L, Algire C, et al. Pharmacological characterization of BAY-876, a novel highly selective inhibitor of glucose transporter (GLUT)-1 in vitro and in vivo[J]. Cancer Research, 2016, 76(14_Supplement): 4746-4746.
[3] Ma Y, Wang W, Idowu M O, et al. Ovarian cancer relies on glucose transporter 1 to fuel glycolysis and growth: anti-tumor activity of BAY-876[J]. Cancers, 2018, 11(1): 33.
[4] Chen Z, Vaeth M, Eckstein M, et al. Characterization of the effect of the GLUT-1 inhibitor BAY-876 on T cells and macrophages[J]. European Journal of Pharmacology, 2023, 945: 175552.
[5] Peshraw Salih Hamadamin, et al. Exploring the anticancer potential of hydrogen sulfide and BAY 876 on clear cell renal cell carcinoma cells: Uncovering novel mutations in VHL and KDR genes among ccRCC patients[J]. Molecular and Clinical Oncology, 2024.
[6] Yang H, Zhang M Z, Sun H, et al. A novel microcrystalline BAY-876 formulation achieves long-acting antitumor activity against aerobic glycolysis and proliferation of hepatocellular carcinoma[J]. Frontiers in Oncology, 2021, 11: 783194.
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Cell experiment [1]: |
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Cell lines |
SKOV-3, OVCAR-3, HEY , A2780 cells |
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Preparation method |
SKOV-3, OVCAR-3, HEY and A2780 cells were treated with BAY-876 (75nM) for 72 hours. |
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Reaction Conditions |
75nM; 72h |
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Applications |
BAY-876 has growth inhibitory effects in SKOV-3, OVCAR-3 and HEY cells but not in A2780 cells. |
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Animal experiment [2]: |
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Animal models |
BalB/c mice |
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Preparation method |
MHCC97-H cells were cultured and injected into nude mice to form the subcutaneous tumor tissues. After MHCC97-H cells form tumor tissues in the subcutaneous position of nude mice, 5mg/kg BAY-876 was given by oral administration every day (once a day for two days). Then, the mice were analyzed by the micro-PET live imaging of small animals,and the tumor tissues were collected for the biochemical analysis. |
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Dosage form |
5mg/kg; p.o. |
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Applications |
BAY-876 significantly inhibits tumor tissue formation and glucose uptake by cells in the tissue. |
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References: |
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| Cas No. | 1799753-84-6 | SDF | |
| Canonical SMILES | O=C(C1=NC2=CC(F)=CC=C2C(C(NC3=C(C)N(CC4=CC=C(C#N)C=C4)N=C3C(F)(F)F)=O)=C1)N | ||
| Formula | C24H16F4N6O2 | M.Wt | 496.42 |
| Solubility | DMSO : ≥ 100 mg/mL (201.44 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| 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 | 2.0144 mL | 10.0721 mL | 20.1442 mL |
| 5 mM | 402.9 μL | 2.0144 mL | 4.0288 mL |
| 10 mM | 201.4 μL | 1.0072 mL | 2.0144 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)