CGP52411
Based on 2 publication(s) in Google Scholar
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
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- Pureté: 99.55%
- CAS No.: 145915-58-8
- Formule: C20H15N3O2
- Masse moléculaire:329.35
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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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CGP52411
MoreVoir tous les produits spécifiques à Isoform EGFR
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Activité biologique
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EGFR 0.3 μM (IC50) |
Amyloid-β |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
>4.5 μM
Compound: 3
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Inhibition of EGF-dependent autophosphorylation of EGF-R in human A431 cells
Inhibition of EGF-dependent autophosphorylation of EGF-R in human A431 cells
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[PMID: 8151612] |
| Balb/MK | IC50 |
11.5 μM
Compound: 3
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Inhibition of BALB/MK mouse epidermal keratinocyte proliferation
Inhibition of BALB/MK mouse epidermal keratinocyte proliferation
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[PMID: 8151612] |
CGP52411 (DAPH; 0-100 μM; 90 minutes; A431 cells) treatment inhibits autophosphorylation and c-src autophosphorylation in vitro in a dose-dependent manner with IC50s of 1 μM and 16 μM, respectively. CGP52411 treatment also shows a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2 with an IC50 value of 10 μM[1].
CGP52411 (DAPH) inhibits c-src kinase with an IC50 value of 16 μM. CGP52411 inhibits PKC isozymes isolated from porcine brain with an IC50 of 80 μM. CGP52411 inhibits conventional PKC isozymes (cPKCs α, β-1, β-2, and γ) but not nonconventional PKC isozymes (nPKCs δ, ε, and ζ) or atypical PKC isozymes (aPKC η)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A431 cells
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Concentration:0 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
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Incubation Time:90 minutes
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Result:Inhibited autophosphorylation in vitro in a dose-dependent manner with an IC50 of 1 μM. c-src autophosphorylation was inhibited with an IC50 of 16 μM. And also resulted in a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2, with an estimated IC50 value of 10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice injected with A431cells[1]
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Dosage:3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg
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Administration:Oral administration; daily; for 15 days
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Result:Antitumor efficacy was obtained at doses between 50 mg/kg and 6.3 mg/kg.
Chemical Information
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CAS No. 145915-58-8
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Appearance Solid
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Masse moléculaire 329.35
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Formule C20H15N3O2
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Color Yellow to orange
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SMILES
O=C1NC(C2=C1C=C(NC3=CC=CC=C3)C(NC4=CC=CC=C4)=C2)=O
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Synonyms
DAPH
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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 (2)
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Journal Impact Factor
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Most Recent
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J Transl Med
Potential of CLSPN as a therapeutic target in melanoma: a key player in melanoma progression and tumor microenvironment. [Abstract]2025 Apr 24;23(1):470. PMID: 40275302 -
Solvant et solubilité
DMSO : 100 mg/mL (303.63 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)
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.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (282 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)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Buchdunger E, et al. 4,5-Dianilinophthalimide: a protein-tyrosine kinase inhibitor with selectivity for the epidermal growth factor receptor signal transduction pathway and potent in vivo antitumor activity. Proc Natl Acad Sci U S A. 1994 Mar 15;91(6):2334-8. [Content Brief]
[2]. Blanchard BJ, et al. Efficient reversal of Alzheimer's disease fibril formation and elimination of neurotoxicity by a small molecule. Proc Natl Acad Sci U S A. 2004 Oct 5;101(40):14326-32. [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 | 3.0363 mL | 15.1814 mL | 30.3628 mL | 75.9071 mL |
| 5 mM | 0.6073 mL | 3.0363 mL | 6.0726 mL | 15.1814 mL | |
| 10 mM | 0.3036 mL | 1.5181 mL | 3.0363 mL | 7.5907 mL | |
| 15 mM | 0.2024 mL | 1.0121 mL | 2.0242 mL | 5.0605 mL | |
| 20 mM | 0.1518 mL | 0.7591 mL | 1.5181 mL | 3.7954 mL | |
| 25 mM | 0.1215 mL | 0.6073 mL | 1.2145 mL | 3.0363 mL | |
| 30 mM | 0.1012 mL | 0.5060 mL | 1.0121 mL | 2.5302 mL | |
| 40 mM | 0.0759 mL | 0.3795 mL | 0.7591 mL | 1.8977 mL | |
| 50 mM | 0.0607 mL | 0.3036 mL | 0.6073 mL | 1.5181 mL | |
| 60 mM | 0.0506 mL | 0.2530 mL | 0.5060 mL | 1.2651 mL | |
| 80 mM | 0.0380 mL | 0.1898 mL | 0.3795 mL | 0.9488 mL | |
| 100 mM | 0.0304 mL | 0.1518 mL | 0.3036 mL | 0.7591 mL |
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