BAY-876

For research use only.

Catalog No.S8452

4 publications

BAY-876 Chemical Structure

CAS No. 1799753-84-6

BAY-876 is a potent and selective GLUT1 inhibitor (IC50=0.002 μM) with a selectivity factor of >100 against GLUT2, GLUT3, and GLUT4.

Selleck's BAY-876 has been cited by 4 publications

Purity & Quality Control

Choose Selective GLUT Inhibitors

Biological Activity

Description BAY-876 is a potent and selective GLUT1 inhibitor (IC50=0.002 μM) with a selectivity factor of >100 against GLUT2, GLUT3, and GLUT4.
Targets
GLUT1 [1]
(Cell-free assay)
0.002 μM
In vitro

BAY-876 is a highly-selective GLUT1 inhibitor with selectivity over GLUT2, 3, and 4 of 4700-, 800-, and 135-fold, respectively[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DLD1 NHvE[oFHfW6ldHnvckBie3OjeR?= M1HIZ|E2KG2rboO= M2O4VGlvcGmkaYTpc44hd2ZiaIXtZY4hT0yXVEGg[ZhxemW|c3XkJIlvKESOREGgZ4VtdHNiYYPz[ZN{\WRiYYOg[4x2[2:|ZTD1dJRic2ViYomgcYVie3W{aX7nJGFVWCCrbnP1ZoF1\WRiZn;yJFE2KG2rboOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiSVO1NEA:KDBwMECyJO69VS5? M1rkbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzN{e0Olc6Lz5|MUe3OFY4QTxxYU6=
Hela-MaTu MkHySpVv[3Srb36gZZN{[Xl? NEXlOVVE\WyudXzhdkBu\WOqYX7pd5Rq[yCjc4PhfVohUW6qaXLpeIlwdiCxZjDncJVkd3OnIIXweIFs\SCkeTDI[YxiNU2jVIWgZ4VtdHNuIFnDOVAhRSByLkCwN|Ih|ryPLh?= NUfWcIVuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDR2OEi5PU8oRkOqRV3CUFww[T5?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 30602670     


Ovarian cancer cell lines were treated with indicated concentrations of BAY-876 for 72 h before the MTT assay to determine the cytotoxic effect of the compound. IC50 in each cell line was calculated.

30602670
Western blot
p-AMPK; 

PubMed: 30602670     


Levels of phosphorylated AMPKα (B) were determined with an ATP bioluminescence assay and immunoblotting analysis, respectively.

30602670
In vivo BAY-876 displays low clearance also in vivo in rat and in dog. The volume of distribution in steady state (Vss) is moderate in both species. Terminal half life is intermediate in rat (2.5 h) and long in dog (22 h) due to the very low clearance. The oral bioavailability (F%) is 85% and 79% in rat and dog, respectively. Preliminary in vivo PK studies of BAY-876 demonstrate that a good oral bioavailability and long terminal half-life is attainable making it an excellent chemical probe to further evaluate the hypothesis of cancer treatment with a very selective GLUT1 inhibitor[1].

Protocol

Solubility (25°C)

In vitro DMSO 99 mg/mL warmed (199.42 mM)
Ethanol 3 mg/mL warmed (6.04 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 496.42
Formula

C24H16F4N6O2

CAS No. 1799753-84-6
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C(=NN1CC2=CC=C(C=C2)C#N)C(F)(F)F)NC(=O)C3=CC(=NC4=C3C=CC(=C4)F)C(=O)N

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID