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

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

CGP52411 Estructura química

No. CAS : 145915-58-8

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of CGP52411:

CGP52411 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CGP52411

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Descripciòn

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

 

Cellular Effect
Cell Line Type Value Description References
A-431 IC50
>4.5 μM
Compound: 3
Inhibition of EGF-dependent autophosphorylation of EGF-R in human A431 cells
Inhibition of EGF-dependent autophosphorylation of EGF-R in human A431 cells
[PMID: 8151612]
Balb/MK IC50
11.5 μM
Compound: 3
Inhibition of BALB/MK mouse epidermal keratinocyte proliferation
Inhibition of BALB/MK mouse epidermal keratinocyte proliferation
[PMID: 8151612]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CGP52411 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Peso molecular

329.35

Fòrmula

C20H15N3O2
No. CAS
Appearance

Solid

Color

Yellow to orange

SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0363 mL 15.1814 mL 30.3628 mL
5 mM 0.6073 mL 3.0363 mL 6.0726 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 99.82%

SDS (392 KB)

COA (255 KB) LCMS (133 KB)

Instrucciones de manejo (2659 KB)
Referencias

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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CGP52411 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CGP52411145915-58-8DAPHCGP 52411CGP-52411EGFRAmyloid-βEpidermal growth factor receptorErbB-1HER1β-amyloid peptideAβAbetaAutophosphorylationc-srcp185c-erbB2antitumororaladministrationAlzheimer'sdiseaseAβ42Inhibitorinhibitorinhibit

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Nombre del producto:
CGP52411
Cat. No.:
HY-103442
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