2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor Tie
  4. BAY-826

BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively.

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

BAY-826 Chemical Structure

BAY-826 Chemical Structure

CAS No. : 1448316-08-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 147 In-stock
Solution
10 mM * 1 mL in DMSO USD 147 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 210 In-stock
25 mg USD 460 In-stock
50 mg USD 820 In-stock
100 mg USD 1480 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

BAY-826 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively.

IC50 & Target

Tie2

1.6 nM (Kd)

In Vitro

BAY-826 is a selective and potent inhibitor of TIE-2 (dissociation constant = 1.6 nM) and binds with similar high affinity to only 4 of 456 tested kinases, namely, TIE-1, DDR1, DDR2, and Serine/threonine-protein kinase 10 (LOK) (dissociation constant = 0.9, 0.4,1.3, and 5.9 nM).The high biochemical affinity for TIE-2 translates into very potent cellular mechanistic activity with an EC50 of about 1.3 nM for inhibition of TIE-2 autophosphorylation in human umbilical vein endothelial cells. The TIE-2 inhibitor BAY-826 is tested for its acute growth inhibitory as well as anti-clonogenic properties in all four mouse glioma cell lines. BAY-826 is highly selective against other angiogenic kinases, such as VEGFR, fibroblast growth factorreceptor (FGFR), or Platelet-derived growth factor receptor (PDGFR), and affects VEGF-stimulated proliferation of HUVEC only atμM concentrations, respectively.

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

BAY-826 Related Antibodies
In Vivo

BAY-826 (oral gavage; 25 mg/kg,50 mg/kg,100 mg/k) potently inhibits ANG-1-stimulated TIE-2 autophosphorylation in murine lungs in female CB17/scid mice[1].
BAY-826 improves tumor control in syngeneic mouse glioma models. Co-treatment with BAY-826 and irradiation is ineffective in one model (SMA-497), but provided synergistic prolongation of survival in another (SMA-560) cell. TIE- 2 inhibition may improve tumor response to treatment in highly vascularized tumors such as glioblastoma[1].

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

558.53

Formula

C26H19F5N6OS
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(NC1=C(C)C=C(C)C(N2C3=CC(C4=CN=CC=C4)=NN3C=C2)=C1)C5=CC(C#N)=CC(S(F)(F)(F)(F)F)=C5
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 (179.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7904 mL 8.9521 mL 17.9041 mL
5 mM 0.3581 mL 1.7904 mL 3.5808 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (1.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1 mg/mL (1.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: 99.94%

COA (252 KB) LCMS (264 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)
References
Cell Assay

Murine SMA-497, SMA-540, SMA-560, and GL-261 glioma cells are used.The cells are commonly cultured as adherent monolayers in Dulbecco`s modified Eagle medium supplemented with 10% heatinactivated fetal calf serum and 2 mM glutamine. Cells are irradiated in a Coradiation source at 1, 3, and 9 Gy. The cells are pre-incubated for 10 min in the 37°C incubator either with 0.1% DMSO as control or 1μM BAY-826. TIE-2 autophosphorylation is induced for 20 min with either 4 mM Na3VO4 or with 400 ng/mL COMP-ANG-1 in the presence of either 0.1% DMSO or 1 μM BAY-826[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration

Following anesthesia, a burr hole is drilled in the skull 2 mm lateral to the bregma. The needle of a Hamilton syringe is introduced to a depth of 3 mm. A volume of 2 μL of a single cell suspension in PBS is slowly injected into the right striatum. In female and male VM/Dk mice (in-house husbandry) 5×10 3 SMA glioma cells are implanted, whereas in female C57Bl/6 mice (Charles River) 2×104 GL-261 cells are implanted (n =10 per group). The mice employed have body weights >20 g. Systemic treatment with BAY-826 is performed by oral gavage (100 mg/kg body weight daily) or the solvent (10% Ethanol/40% Solutol/50% Aqua dest), respectively [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
DMSO 1 mM 1.7904 mL 8.9521 mL 17.9041 mL 44.7604 mL
5 mM 0.3581 mL 1.7904 mL 3.5808 mL 8.9521 mL
10 mM 0.1790 mL 0.8952 mL 1.7904 mL 4.4760 mL
15 mM 0.1194 mL 0.5968 mL 1.1936 mL 2.9840 mL
20 mM 0.0895 mL 0.4476 mL 0.8952 mL 2.2380 mL
25 mM 0.0716 mL 0.3581 mL 0.7162 mL 1.7904 mL
30 mM 0.0597 mL 0.2984 mL 0.5968 mL 1.4920 mL
40 mM 0.0448 mL 0.2238 mL 0.4476 mL 1.1190 mL
50 mM 0.0358 mL 0.1790 mL 0.3581 mL 0.8952 mL
60 mM 0.0298 mL 0.1492 mL 0.2984 mL 0.7460 mL
80 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5595 mL
100 mM 0.0179 mL 0.0895 mL 0.1790 mL 0.4476 mL
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BAY-826 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-8261448316-08-2BAY826BAY 826Discoidin Domain ReceptorTieAngiopoietin receptorInhibitorinhibitorinhibit

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