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.

For research use only. We do not sell to patients.

CGP52411 Chemical Structure

CGP52411 Chemical Structure

CAS No. : 145915-58-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 107 In-stock
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10 mM * 1 mL in DMSO USD 107 In-stock
Solid
1 mg USD 39 In-stock
5 mg USD 98 In-stock
10 mg USD 151 In-stock
25 mg USD 303 In-stock
50 mg USD 455 In-stock
100 mg USD 660 In-stock
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Based on 1 publication(s) in Google Scholar

CGP52411 Related Antibodies

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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].

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.
Molecular Weight

329.35

Formula

C20H15N3O2
CAS No.
Appearance

Solid

Color

Yellow to orange

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.82%

COA (255 KB) LCMS (133 KB)

Handling Instructions (2659 KB)
References

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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