PD158780
Based on 4 publication(s) in Google Scholar
PD158780 is a potent EGFR family inhibitor with IC50s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.47%
- CAS. Nr.: 171179-06-9
- Formel: C14H12BrN5
- Molecular Weight:330.18
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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- Reinheit & Dokumentation
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PD158780
MoreAlle EGFR Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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EGFR 8 μM (IC50, Cell Assay) |
ErbB2 49 nM (IC50, Cell Assay) |
ErbB3 52 nM (IC50, Cell Assay) |
ErbB4 52 nM (IC50, Cell Assay) |
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Cell Line
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Type | Value | Description | References |
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| A-431 | IC50 |
0.008 nM
Compound: 7f
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Inhibitory potency against isolated epidermal growth factor receptor (EGFR) from human A431 carcinoma cells
Inhibitory potency against isolated epidermal growth factor receptor (EGFR) from human A431 carcinoma cells
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[PMID: 8627606] |
| A-431 | IC50 |
0.008 nM
Compound: Table 2 A-OMe
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Tested for inhibition of PLC gamma-derived substrate in Epidermal growth factor receptor stimulated A431 cells
Tested for inhibition of PLC gamma-derived substrate in Epidermal growth factor receptor stimulated A431 cells
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[PMID: 9191958] |
| A-431 | IC50 |
13 nM
Compound: 5b
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Inhibition of autophosphorylation of epidermal growth factor receptor in A431 cells in culture
Inhibition of autophosphorylation of epidermal growth factor receptor in A431 cells in culture
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[PMID: 9513602] |
| A-431 | IC50 |
13 μM
Compound: 5b
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Inhibition of EGF-dependent autophosphorylation of EGF-R in A431 cells
Inhibition of EGF-dependent autophosphorylation of EGF-R in A431 cells
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[PMID: 9513602] |
| A-431 | IC50 |
15 nM
Compound: 7f
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Inhibition of Epidermal growth factor receptor autophosphorylation in A431 human epidermoid carcinoma cells
Inhibition of Epidermal growth factor receptor autophosphorylation in A431 human epidermoid carcinoma cells
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[PMID: 8627606] |
| A-431 | IC50 |
15 nM
Compound: Table 2 A-OMe
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Tested for inhibition of autophosphorylation in Epidermal growth factor receptor stimulated A431 cells
Tested for inhibition of autophosphorylation in Epidermal growth factor receptor stimulated A431 cells
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[PMID: 9191958] |
| MDA-MB-453 | IC50 |
52 μM
Compound: 5b
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Inhibition of heregulin-dependent autophosphorylation of ErbB2 receptor in MDA-MB-453 cells
Inhibition of heregulin-dependent autophosphorylation of ErbB2 receptor in MDA-MB-453 cells
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[PMID: 9513602] |
PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC50 value of 13 nM. PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulin-stimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC50 values of 49 and 52 nM, respectively, suggesting that the compound is active against other members of the EGF receptor family[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 171179-06-9
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Appearance Solid
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Molecular Weight 330.18
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Formel C14H12BrN5
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Color Light yellow to yellow
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SMILES
CNC1=CC2=C(NC3=CC(Br)=CC=C3)N=CN=C2C=N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Diabetes Obes Metab
Neuregulin4-ErbB4 signalling pathway is driven by electroacupuncture stimulation to remodel brown adipose tissue innervation. [Abstract]2024 Sep;26(9):3880-3896. PMID: 38951947 -
Mol Neurobiol
Htr2b Promotes M1 Microglia Polarization and Neuroinflammation after Spinal Cord Injury via Inhibition of Neuregulin-1/ErbB Signaling. [Abstract]2024 Mar;61(3):1643-1654. PMID: 37747614
Lösungsmittel & Löslichkeit
DMSO : 16.67 mg/mL (50.49 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: 1.67 mg/mL (5.06 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1.67 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: 1.67 mg/mL (5.06 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
Protokoll
The enzyme assay is performed in 96-well filter plates. The total volume is 0.1 mL containing 20 mM HEPES, pH 7.4, 50 μM sodium vanadate, 40 mM magnesium chloride, 10 μM ATP containing 0.5 μCi of [32p]ATP, 20 μg of polyglutamic acid/tyrosine, 1 ng of EGF receptor tyrosine kinase, ard appropriate dilutions of inhibitor (PD158780) and/or ATP. All corrtponents except the ATP are added to the well, and the plate is incubated with shaking for 10 min at 25°C. The reaction is started by adding [32p]ATP, and the plate is incubated with shaking at 25°C for 10 min. The reaction is terminated by the addition of 0.1 mL of 20% TCA, and the plate is kept at 4°C for at least 15 min to allow the substrate to precipitate. The wells are then ished five times with 0.125 mL of 10% TCA, and [32p] incorporation is determined[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
All cell lines are maintained as monolayers in dMEM/F12, 50:50 containing 10% fetal bovine serum. For growth inhibition assays, dilutions of the designated compound (PD158780) in 10 μL are placed in 24-well plates followed by the addition of cells in 2 mL of medium. The plates are incubated for 72 hr at 37°C in a humidified atmosphere. Cell growth is determined by counting cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tumor fragments were implanted sc into the right axilla of mice on day 0. PD158780 is administered intraperitoneally or orally. Tumor growth is monitored[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 3.0287 mL | 15.1433 mL | 30.2865 mL | 75.7163 mL |
| 5 mM | 0.6057 mL | 3.0287 mL | 6.0573 mL | 15.1433 mL | |
| 10 mM | 0.3029 mL | 1.5143 mL | 3.0287 mL | 7.5716 mL | |
| 15 mM | 0.2019 mL | 1.0096 mL | 2.0191 mL | 5.0478 mL | |
| 20 mM | 0.1514 mL | 0.7572 mL | 1.5143 mL | 3.7858 mL | |
| 25 mM | 0.1211 mL | 0.6057 mL | 1.2115 mL | 3.0287 mL | |
| 30 mM | 0.1010 mL | 0.5048 mL | 1.0096 mL | 2.5239 mL | |
| 40 mM | 0.0757 mL | 0.3786 mL | 0.7572 mL | 1.8929 mL | |
| 50 mM | 0.0606 mL | 0.3029 mL | 0.6057 mL | 1.5143 mL |
PD158780 Related Classifications
HY-18609 Related Classifications
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