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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.55%
- CAS 番号: 145915-58-8
- 分子式: C20H15N3O2
- 分子量:329.35
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 CGP52411
MoreEGFR アイソフォーム固有の製品をすべて表示
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生物活性
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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.
化学情報
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CAS 番号 145915-58-8
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性状 Solid
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分子量 329.35
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分子式 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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別名
DAPH
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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 -
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (282 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
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- Portuguese - PT (392 KB)
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取扱説明書 (2659 KB)
参考文献
[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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