BAY-876

Catalog No.S8452

For research use only.

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

BAY-876 Chemical Structure

CAS No. 1799753-84-6

Selleck's BAY-876 has been cited by 5 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
Hela-MaTu M3L3VWZ2dmO2aX;uJIF{e2G7 M3r3UmNmdGy3bHHyJI1m[2ijbnnzeIlkKGG|c3H5PkBKdmirYnn0bY9vKG:oIHfseYNwe2VidYD0ZYtmKGK7IFjlcIEuVWGWdTDj[YxteyxiSVO1NEA:KDBwMECzNkDPxE1w NFHzUIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PDR6OEm5M{c,S2iHTVLMQE9iRg>?
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 30602670
Western blot p-AMPK 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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 496.42
Formula

C24H16F4N6O2

CAS No. 1799753-84-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
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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 ddH2O, 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.

Molarity Calculator

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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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