Cat. No.: HY-103442

CGP52411

(Synonyms: DAPH)

2 Cited Publications

고객리뷰

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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Purity: 99.55%
CAS No.: 145915-58-8
화학식: C₂₀H₁₅N₃O₂
분자량:329.35

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CGP52411 Chemical Structure

CAS No.: 145915-58-8

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Antibody-Drug Conjugates

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]^[2]

EGFR

0.3 μM (IC₅₀)

Amyloid-β

All EGFR Isoforms :

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.

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 p^185c-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.

Chemical Information

CAS No. 145915-58-8
Appearance Solid
분자량 329.35
화학식 C₂₀H₁₅N₃O₂
Color Yellow to orange
SMILES

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

DAPH
선적

Room temperature in continental US; may vary elsewhere.

보관

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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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
bioRxiv

2026 May 7.

용액&용해도

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0363 mL

15.1814 mL

30.3628 mL

5 mM

0.6073 mL

3.0363 mL

6.0726 mL

10 mM

0.3036 mL

1.5181 mL

3.0363 mL

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.

몰농도 계산기

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

Mass

Concentration

Volume

Molecular Weight

농도 희석 계산기

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) CGP52411

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (2)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

CGP52411 Related Classifications

Cat. No.: HY-103442