BAY-826
Based on 1 publication(s) in Google Scholar
BAY-826, a chemical probe, is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively.
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- Pureté: 99.94%
- CAS No.: 1448316-08-2
- Formule: C26H19F5N6OS
- Masse moléculaire:558.53
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Solvant et solubilité
- Protocole
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) BAY-826
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Activité biologique
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Tie2 1.6 nM (Kd) |
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 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.
Chemical Information
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CAS No. 1448316-08-2
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Appearance Solid
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Masse moléculaire 558.53
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Formule C26H19F5N6OS
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Color White to yellow
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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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