GW779439X
Based on 1 publication(s) in Google Scholar
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
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- Pureza: 99.85%
- No. CAS: 551919-98-3
- Fòrmula: C22H21F3N8
- Peso molecular:454.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GW779439X
MoreVer todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
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Aurora A |
Stk1 |
apoptosis |
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Cell Line
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Type | Value | Description | References |
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| BT-474 | IC50 |
1130 nM
Compound: CICAMPA-06
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Cytotoxicity against human BT-474 cells incubated for 48 hrs by CCK-8 reagent microplate reader assay
Cytotoxicity against human BT-474 cells incubated for 48 hrs by CCK-8 reagent microplate reader assay
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[PMID: 36827953] |
| THP-1 | CC50 |
<0.05 μM
Compound: 1, GW779439X
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Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 35035774] |
GW779439X (2 μM) biochemically inhibits Stk1. GW779439X (5 μM) potentiates ceftaroline activity against a ceftaroline-resistant MRSA strain. GW779439X is able to potentiate the activity of oxacillin against various S. aureus isolates, including both MRSA and MSSA isolates, but the potentiation is clearly strongest in PBP2A-containing strains[1].
GW779439X has growth inhibition effects on the AGP-01 cell line (IC50= 0.57 μM). GW779439X (1μM) significantly blockS the cell cycle at the G0/G1 phase and sub-G1 phase. GW779439X (1μM; 72 hours; AGP-01 cells) significantly decreases expression levels of genes involved in proliferation progression (c-MYC, NRAS, and CDC25A) and increases expression levels of genes involved in cell cycle blocking (CDKN1A and TP53)[2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 551919-98-3
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Appearance Solid
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Peso molecular 454.45
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Fòrmula C22H21F3N8
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Color White to light brown
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SMILES
FC(C1=CC(NC2=NC=CC(C3=C4C=CC=NN4N=C3)=N2)=CC=C1N5CCN(C)CC5)(F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Res Sq
Stk1 is required for BlaR1-mediated broad-spectrum β-lactam resistance in epidemic-causing strains of Staphylococcus aureus. [Abstract]2026 Jan 12:rs.3.rs-8331258. PMID: 41743328
Solvente y solubilidad
DMSO : 31.25 mg/mL (68.76 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: ≥ 3.33 mg/mL (7.33 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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: ≥ 3.33 mg/mL (7.33 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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.
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Mesquita FP, et al. Kinase inhibitor screening reveals aurora-a kinase is a potential therapeutic and prognostic biomarker of gastric cancer [published online ahead of print, 2021 Jun 23]. J Cell Biochem. 2021;10.1002/jcb.30015. [Content Brief]
[2]. Schaenzer AJ, et al. GW779439X and Its Pyrazolopyridazine Derivatives Inhibit the Serine/Threonine Kinase Stk1 and Act As Antibiotic Adjuvants against β-Lactam-Resistant Staphylococcus aureus. ACS Infect Dis. 2018;4(10):1508-1518. [Content Brief]
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 | 2.2005 mL | 11.0023 mL | 22.0046 mL | 55.0116 mL |
| 5 mM | 0.4401 mL | 2.2005 mL | 4.4009 mL | 11.0023 mL | |
| 10 mM | 0.2200 mL | 1.1002 mL | 2.2005 mL | 5.5012 mL | |
| 15 mM | 0.1467 mL | 0.7335 mL | 1.4670 mL | 3.6674 mL | |
| 20 mM | 0.1100 mL | 0.5501 mL | 1.1002 mL | 2.7506 mL | |
| 25 mM | 0.0880 mL | 0.4401 mL | 0.8802 mL | 2.2005 mL | |
| 30 mM | 0.0733 mL | 0.3667 mL | 0.7335 mL | 1.8337 mL | |
| 40 mM | 0.0550 mL | 0.2751 mL | 0.5501 mL | 1.3753 mL | |
| 50 mM | 0.0440 mL | 0.2200 mL | 0.4401 mL | 1.1002 mL | |
| 60 mM | 0.0367 mL | 0.1834 mL | 0.3667 mL | 0.9169 mL |
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