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| Targets |
CGP52411 targets the epidermal growth factor receptor (EGFR), specifically inhibiting its intracellular kinase domain. It acts as an ATP-competitive inhibitor, binding to the ATP-binding pocket of the kinase and preventing phosphorylation of downstream signaling proteins. This inhibits EGFR-mediated signal transduction pathways involved in cell proliferation and survival. It also blocks the toxic influx of Ca²⁺ ions into neuronal cells.
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| ln Vitro |
In vitro, autophosphorylation and c-src autophosphorylation are inhibited in a dose-dependent manner with IC50 values of 1 μM and 16 μM, respectively, upon treatment with CGP52411 (DAPH; 0-100 μM; 90 min; A431 cells). Moreover, p185c-erbB2 tyrosine phosphorylation decreased concentration-dependently after CGP52411 treatment, with an IC50 value of 10 μM [1]. At an IC50 of 16 μM, CGP52411 (DAPH) inhibits c-src kinase. With an IC50 of 80 μM, CGP52411 inhibits the PKC isoenzyme that was isolated from swine brain. PKC isoenzymes that are conventional (cPKC α, β-1, β-2, and γ) are inhibited by CGP52411, while those that are atypical (aPKC η) or unconventional (nPKC δ, ε, and ζ) are not [1].
In vitro, CGP52411 selectively inhibits the EGFR kinase domain with an IC50 of 0.3 μM. It has also been shown to dramatically inhibit and reverse the formation of β-amyloid (Aβ42) fibril aggregates. The compound blocks the toxic influx of Ca²⁺ ions into neuronal cells, suggesting a neuroprotective mechanism. It is a potent, selective, and orally active research tool. |
| ln Vivo |
CGP52411 targets xenografts in vivo and shows anti-tumor action (3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg; oral dose; daily; for 15 days; female BALB/c nude mice) [1].
CGP52411 is an orally active compound that has demonstrated potent in vivo antitumor activity. Its ability to inhibit EGFR signaling translates to efficacy in animal models of cancer. It is also being investigated in Alzheimer's disease research due to its effects on Aβ42 aggregation and Ca²⁺ signaling. The compound's in vivo profile makes it a valuable tool for studying EGFR and Aβ pathology in preclinical models. |
| Enzyme Assay |
In vitro enzyme assays for CGP52411 involve EGFR kinase inhibition studies. The kinase is incubated with increasing concentrations of the compound, ATP, and a specific peptide substrate in kinase assay buffer. Phosphorylation of the substrate is measured using radioactive ³³P-ATP or through luminescence-based assays. IC50 values are calculated from dose-response curves. Selectivity profiling is performed using a panel of kinases to confirm its specificity for EGFR.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: A431 Cell Tested Concentrations: 0 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM Incubation Duration: 90 min Experimental Results: Inhibition of autophosphorylation in a dose-dependent manner in vitro, IC50 1μM. c-src autophosphorylation is inhibited with an IC50 of 16 μM. It also resulted in a concentration-dependent decrease in tyrosine phosphorylation of p185c-erbB2, with an estimated IC50 value of 10 μM. For in vitro cell-based assays, cancer cell lines that are dependent on EGFR signaling (e.g., A431, MDA-MB-468) are cultured. Cells are treated with CGP52411, and EGFR phosphorylation is measured by Western blot. Cell proliferation and viability are assessed by MTT or CellTiter-Glo assays. For neuroprotection studies, neuronal cells are treated with Aβ42 in the presence of the compound, and cell viability and Ca²⁺ influx are measured using fluorescent indicators. |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice injected with A431 cells [1]
Doses: 3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, 50 mg/kg Route of Administration: Oral; Oral; Injection Medication. Daily; continued for 15 days Experimental Results: Antitumor efficacy was obtained at doses of 50 mg/kg to 6.3 mg/kg. In vivo animal studies with CGP52411 typically use mouse xenograft models of EGFR-driven cancers. Tumors are implanted subcutaneously, and the compound is administered orally. Tumor volume is monitored. For Alzheimer's research, transgenic mouse models of amyloidosis are used. The compound's ability to reduce Aβ plaque load and improve cognitive function is assessed through behavioral tests and immunohistochemistry. |
| ADME/Pharmacokinetics |
CGP52411 (CAS: 145915-58-8) has a molecular weight of 329.35 g/mol and a molecular formula of C20H15N3O2. It is also known as 4,5-Dianilinophthalimide. It is a solid with a purity of ≥99% and is stored at room temperature. The compound is soluble in DMSO. It is a highly selective, orally active, and ATP-competitive EGFR inhibitor.
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| Toxicity/Toxicokinetics |
CGP52411 is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile, though comprehensive toxicology data are limited. As an EGFR inhibitor, it may have effects on normal tissues that express EGFR. However, its selectivity suggests a favorable therapeutic window. Standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
4,5-Diphenylaminophthalimide is a phthalimide in which aniline groups are substituted at the 4 and 5 positions. It possesses tyrosine kinase inhibitor and anti-aging properties.
CGP52411 is a highly selective, orally active, and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. It is also known as DAPH. It has shown potential in both oncology and Alzheimer's disease research. It is not FDA-approved and is intended for research use only. |
| Molecular Formula |
C₂₀H₁₅N₃O₂MOLECULARWEIGHT
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| Molecular Weight |
329.35
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| Exact Mass |
329.116
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| Elemental Analysis |
C, 72.94; H, 4.59; N, 12.76; O, 9.72
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| CAS # |
145915-58-8
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| PubChem CID |
1697
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| Appearance |
Yellow to orange solid powder
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| Density |
1.374 g/cm3
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| Melting Point |
199-202℃
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| LogP |
4.532
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
453
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1NC(=O)C2=CC(=C(C=C12)NC1C=CC=CC=1)NC1C=CC=CC=1
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| InChi Key |
AAALVYBICLMAMA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15N3O2/c24-19-15-11-17(21-13-7-3-1-4-8-13)18(12-16(15)20(25)23-19)22-14-9-5-2-6-10-14/h1-12,21-22H,(H,23,24,25)
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| Chemical Name |
5,6-dianilinoisoindole-1,3-dione
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| Synonyms |
CGP52411; CGP-52411
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~303.63 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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