| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
BAY-876 (BAY876) is a potent and highly-selective GLUT1 (SLC2A1) inhibitor with potential anticancer activity. It inhibits GLUT1 with an IC50 of 2 nM and exhibits high selectivity over GLUT2, 3, and 4 (4700-, 800-, and 135-fold, respectively). BAY-876 exhibited good metabolic stability in vitro and high oral bioavailability in vivo. GLUT1 overexpression has been reported in many types of human cancers, including those of brain,6 breast, colon, kidney, lung, ovary, and prostate, and is correlated with advanced cancer stages and poor clinical outcomes. Despite the long-known fact that the facilitative glucose transporter GLUT1 is one of the key players safeguarding the increase in glucose consumption of many tumor entities even under conditions of normal oxygen supply (known as the Warburg effect), only few endeavors have been undertaken to find a GLUT1-selective small-molecule inhibitor.
| ln Vitro |
Growth inhibitory BAY-876 (25–75 nM; 24 and 72 hours) reduces the number of SKOV-3 and OVCAR-3 cells in a dose-dependent manner [2].
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| ln Vivo |
Mice treated orally with BAY-876 (1.5–4.5 mg/kg/day for 28 days) showed a notable dose-dependent reduction in carcinogenicity [2].
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: SKOV-3 and OVCAR-3 cells Tested Concentrations: 25, 50, 75 nM Incubation Duration: 24 and 72 hrs (hours) Experimental Results: Led to a dose-dependent decrease in numbers of SKOV-3 and OVCAR- 3 cells. |
| Animal Protocol |
Animal/Disease Models: Female NOD-scid IL2rgnull (NSG) mice carrying SKOV-3 subcutaneous (sc) xenografts[2]
Doses: 1.5, 3, 4.5 mg/kg Route of Administration: Oral administration; daily; for 28 days Experimental Results: Caused a clear dose -dependent inhibition of tumorigenicity. |
| References |
[1]. Siebeneicher H et al. Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876. ChemMedChem. 2016 Aug 23.
[2]. Ma Y, et al. Ovarian Cancer Relies on Glucose Transporter 1 to Fuel Glycolysis and Growth: Anti-Tumor Activity of BAY-876. Cancers (Basel). 2018 Dec 31;11(1). |
| Molecular Formula |
C24H16F4N6O2
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| Molecular Weight |
496.42
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| CAS # |
1799753-84-6
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| SMILES |
O=C(C1=NC2=CC(F)=CC=C2C(C(NC3=C(C)N(CC4=CC=C(C=C4)C#N)N=C3C(F)(F)F)=O)=C1)N
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 5 mg/mL (10.07 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0144 mL | 10.0721 mL | 20.1442 mL | |
| 5 mM | 0.4029 mL | 2.0144 mL | 4.0288 mL | |
| 10 mM | 0.2014 mL | 1.0072 mL | 2.0144 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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