AG-825
Based on 1 publication(s) in Google Scholar
AG-825 is a selective, ATP-competitive, tyrosine phosphorylation ErbB2 inhibitor with an IC50 of 0.35 μM. AG825 significantly accelerates Apoptosis of human neutrophils. AG-825 increases β1AR density. AAG-825 has anticancer and anti-inflammatory activities. AAG-825 can be used in cardiovascular disease research.
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- Pureza: 98.13%
- No. CAS: 149092-50-2
- Fòrmula: C19H15N3O3S2
- Peso molecular:397.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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GPCR/G Protein Compound Library
HY-L006
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Immunology/Inflammation Compound Library
HY-L007
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JAK/STAT Compound Library
HY-L008
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Kinase Inhibitor Library
HY-L009
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Neuronal Signaling Compound Library
HY-L013
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Protein Tyrosine Kinase Compound Library
HY-L016
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Anti-Cancer Compound Library
HY-L025
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Covalent Screening Library
HY-L036
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Differentiation Inducing Compound Library
HY-L038
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Neurotransmitter Receptor Compound Library
HY-L062
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Anti-Hepatitis C Virus Compound Library
HY-L073
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Lung Cancer Compound Library
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Anti-Pancreatic Cancer Compound Library
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Membrane Receptor-targeted Compound Library
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Cysteine Targeted Covalent Library
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Highly Selective Inhibitors Library
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Highly Selective Activators Library
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Publications Citing Use of MedChemExpress (MCE) AG-825
MoreVer todos los productos específicos de isoformas EGFR
MoreVer todos los productos específicos de isoformas Adrenergic Receptor
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Actividad biológica
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ErbB2 0.35 μM (IC50) |
EGFR 19 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HCC1954 | IC50 |
30 μM
Compound: AG825
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Antiproliferative activity against human HCC1954 cells measured after 72 hrs by SRB assay
Antiproliferative activity against human HCC1954 cells measured after 72 hrs by SRB assay
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[PMID: 34844036] |
| NIH3T3 | IC50 |
35 μM
Compound: 15
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Inhibition of HER-14 (human EGFR overexpressing NIH3T3) cell proliferation
Inhibition of HER-14 (human EGFR overexpressing NIH3T3) cell proliferation
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[PMID: 7902440] |
AG-825 (72 h) shows antiproliferative activity against human HCC1954 cells, with IC50 of 30 μM[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AG-825 (1 mg/kg, min-osmotic pump, 14 days) causes cardiac dilation and selective increase in β1AR density in mice[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine model of LPS induced acute lung inflammation[4]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Had no effect on percentage of, or absolute number of neutrophils or macrophages.
Increased the percentage of neutrophil apoptosis.
Elevated macrophage efferocytosis.
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Animal Model:Murine model of Zymosan (HY-159069)-induced peritonitis[4]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Did not induce leukopenia.
Showed fewer inflammatory cells in peritoneal lavage.
Reduced the neutrophil chemoattractant and proinflammatory cytokine, KC.
Reduced IgM.
Chemical Information
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No. CAS 149092-50-2
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Appearance Solid
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Peso molecular 397.47
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Fòrmula C19H15N3O3S2
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Color Light yellow to yellow
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SMILES
O=C(N)/C(C#N)=C/C1=CC(OC)=C(O)C(CSC2=NC3=CC=CC=C3S2)=C1
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Synonyms
Tyrphostin AG-825
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Pflugers Arch
Unlocking the potential: unveiling tyrphostins with Michael-reactive cyanoacrylate motif as promising inhibitors of human 5-lipoxygenase. [Abstract]2024 Dec;476(12):1913-1928. PMID: 39347835
Solvente y solubilidad
DMSO : 250 mg/mL (628.98 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (279 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wolfson E, et al. Nucleolin and ErbB2 inhibition reduces tumorigenicity of ErbB2-positive breast cancer. Cell Death Dis. 2018 Jan 19;9(2):47. [Content Brief]
[2]. Gazit A, et al. Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins. J Med Chem. 1993 Nov 12;36(23):3556-64. [Content Brief]
[3]. He H, et al. Signal therapy for RAS-induced cancers in combination of AG 879 and PP1, specific inhibitors for ErbB2 and Src family kinases, that block PAK activation. Cancer J. 2001 May-Jun;7(3):191-202. [Content Brief]
[4]. Rahman A, et al. Inhibition of ErbB kinase signalling promotes resolution of neutrophilic inflammation. Elife. 2019 Oct 15;8. pii: e50990. [Content Brief]
[5]. Ling J, et al. Identifying key genes, pathways and screening therapeutic agents for manganese-induced Alzheimer disease using bioinformatics analysis. Medicine (Baltimore). 2018 Jun;97(22):e10775. [Content Brief]
[6]. Piven YA, et al. Novel O-acylated (E)-3-aryl-6,7-dihydrobenzisoxazol-4(5H)-one oximes targeting HSP90-HER2 axis in breast cancer cells. Bioorg Med Chem. 2022 Jan 1;53:116521. [Content Brief]
[7]. Gupta MK, et al. Anthracycline Cardiotoxicity Is Associated With Elevated β1-Adrenergic Receptor Density. J Am Heart Assoc. 2022 Feb 15;11(4):e023457. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5159 mL | 12.5796 mL | 25.1591 mL | 62.8978 mL |
| 5 mM | 0.5032 mL | 2.5159 mL | 5.0318 mL | 12.5796 mL | |
| 10 mM | 0.2516 mL | 1.2580 mL | 2.5159 mL | 6.2898 mL | |
| 15 mM | 0.1677 mL | 0.8386 mL | 1.6773 mL | 4.1932 mL | |
| 20 mM | 0.1258 mL | 0.6290 mL | 1.2580 mL | 3.1449 mL | |
| 25 mM | 0.1006 mL | 0.5032 mL | 1.0064 mL | 2.5159 mL | |
| 30 mM | 0.0839 mL | 0.4193 mL | 0.8386 mL | 2.0966 mL | |
| 40 mM | 0.0629 mL | 0.3145 mL | 0.6290 mL | 1.5724 mL | |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.2580 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4193 mL | 1.0483 mL | |
| 80 mM | 0.0314 mL | 0.1572 mL | 0.3145 mL | 0.7862 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6290 mL |
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