2. Membrane Transporter/Ion Channel
  3. GLUT
  4. BAY-876

BAY-876 est un inhibiteur puissant, sélectif du transporteur de glucose 1 (GLUT1) et oralement actif avec un IC50 de 2 nM. BAY-876 est> 130 fois plus sélectif pour GLUT1 que GLUT2, GLUT3 et GLUT4. BAY-876 est également un inhibiteur puissant du métabolisme glycolytique et de la croissance du cancer de l'ovaire.

BAY-876 ist ein potenter, selektiver und oral wirksamer glucose transporter 1 (GLUT1)-Inhibitor mit einem IC50 von 2 nM. BAY-876 ist >130-mal selektiver für GLUT1 als GLUT2, GLUT3 und GLUT4. BAY-876 ist auch ein potenter Blocker des glykolytischen Stoffwechsels und des Ovarialkarzinom-Wachstums.

BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth.

For research use only. We do not sell to patients.

BAY-876 Chemical Structure

BAY-876 Chemical Structure

CAS No. : 1799753-84-6

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10 mM * 1 mL in DMSO
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Solid
2 mg USD 96 In-stock
5 mg USD 120 In-stock
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Based on 17 publication(s) in Google Scholar

BAY-876 Related Antibodies

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GLUT1 GLUT2 GLUT3 GLUT4

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Description

BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4[1]. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth[2].

IC50 & Target[1]

GLUT1

2 nM (IC50)

GLUT2

10.08 μM (IC50)

GLUT3

1.67 μM (IC50)

GLUT4

0.29 μM (IC50)

In Vitro

BAY-876 (25-75 nM; 24 and 72 hours) has the growth-inhibitory effect and leads to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BAY-876 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: SKOV-3 and OVCAR-3 cells
Concentration: 25, 50, 75 nM
Incubation Time: 24 and 72 hours
Result: Led to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells.
In Vivo

BAY-876 (oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition of tumorigenicity in mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD-scid IL2rgnull (NSG) mice carrying SKOV-3 subcutaneous (s.c.) xenografts[2]
Dosage: 1.5, 3, 4.5 mg/kg
Administration: Oral administration; daily; for 28 days
Result: Caused a clear dose-dependent inhibition of tumorigenicity.
Molecular Weight

496.42

Formula

C24H16F4N6O2
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (201.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Methanol : 1 mg/mL (2.01 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 5 mg/mL (10.07 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.46%

COA (259 KB) HNMR (180 KB) LCMS (349 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Methanol / DMSO 1 mM 2.0144 mL 10.0721 mL 20.1442 mL 50.3606 mL
DMSO 5 mM 0.4029 mL 2.0144 mL 4.0288 mL 10.0721 mL
10 mM 0.2014 mL 1.0072 mL 2.0144 mL 5.0361 mL
15 mM 0.1343 mL 0.6715 mL 1.3429 mL 3.3574 mL
20 mM 0.1007 mL 0.5036 mL 1.0072 mL 2.5180 mL
25 mM 0.0806 mL 0.4029 mL 0.8058 mL 2.0144 mL
30 mM 0.0671 mL 0.3357 mL 0.6715 mL 1.6787 mL
40 mM 0.0504 mL 0.2518 mL 0.5036 mL 1.2590 mL
50 mM 0.0403 mL 0.2014 mL 0.4029 mL 1.0072 mL
60 mM 0.0336 mL 0.1679 mL 0.3357 mL 0.8393 mL
80 mM 0.0252 mL 0.1259 mL 0.2518 mL 0.6295 mL
100 mM 0.0201 mL 0.1007 mL 0.2014 mL 0.5036 mL
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BAY-876 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAY-8761799753-84-6BAY876BAY 876GLUTGlucose transporterorallyglucosetransporter1glycolyticmetabolismovariancancerInhibitorinhibitorinhibit

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