CGP52411 (Synonyms: DAPH)

Name: CGP52411
Brand: MedChemExpress
SKU: HY-103442
Rating: 4.5 (1 reviews)

Cat. No.: HY-103442 Purity: 99.71%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 145915-58-8

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 107	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 107	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 98	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 151	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 303	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 455	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 660	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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.

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.

Molecular Weight

329.35

Formula

C₂₀H₁₅N₃O₂

CAS No.

145915-58-8

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
10 mM	0.3036 mL	1.5181 mL	3.0363 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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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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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%

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Data Sheet (281 KB) SDS (252 KB)

COA (255 KB) LCMS (133 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]

Complete Stock Solution Preparation Table

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

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.

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CGP52411 (Synonyms: DAPH)

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Complete Stock Solution Preparation Table

CGP52411 Related Classifications

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