1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Neuronal Signaling
  2. EGFR
    Amyloid-β
  3. CGP52411

CGP52411 (Synonyms: DAPH)

Cat. No.: HY-103442
Handling Instructions

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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CGP52411 Chemical Structure

CGP52411 Chemical Structure

CAS No. : 145915-58-8

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10 mM * 1 mL in DMSO USD 478 In-stock
Estimated Time of Arrival: December 31
1 mg USD 220 In-stock
Estimated Time of Arrival: December 31
5 mg USD 660 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target[1][2]

EGFR

0.3 μM (IC50)

Amyloid-β

 

In Vitro

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].

Western Blot Analysis[1]

Cell Line: A431 cells
Concentration: 0 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
Incubation Time: 90 minutes
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.
In Vivo

CGP52411 (3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg; oral administration; daily; for 15 days; female BALB/c nude mice) treatment in vivo against xenografts of the A431 and SK-OV-3 tumors, and has antitumor activity[1].

Animal Model: Female BALB/c nude mice injected with A431cells[1]
Dosage: 3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg
Administration: Oral administration; daily; for 15 days
Result: Antitumor efficacy was obtained at doses between 50 mg/kg and 6.3 mg/kg.
Molecular Weight

329.35

Formula

C₂₀H₁₅N₃O₂

CAS No.

145915-58-8

SMILES

O=C1NC(C2=C1C=C(NC3=CC=CC=C3)C(NC4=CC=CC=C4)=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CGP52411DAPHCGP 52411CGP-52411EGFRAmyloid-βEpidermal growth factor receptorErbB-1HER1β-amyloid peptideAbetaAutophosphorylationc-srcp185c-erbB2antitumororaladministrationAlzheimer'sdiseaseAβ42Inhibitorinhibitorinhibit

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CGP52411
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