[CAS NO. 145915-58-8] CGP52411
PRODUCTS SPECIFICATIONS [145915-58-8]
DESCRIPTION [145915-58-8]
Overview
| MDL | MFCD00236442 |
|---|---|
| Molecular Weight | 329.35 |
| Molecular Formula | C20H15N3O2 |
| SMILES | O=C1NC(C2=C1C=C(NC3=CC=CC=C3)C(NC4=CC=CC=C4)=C2)=O |
Summary
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC 50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ 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
|
EGFR 0.3 μM (IC 50 ) |
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
IC
50
s of 1 μM and 16 μM, respectively. CGP52411 treatment also shows a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2 with an
IC
50
value of 10 μM
[1]
.
CGP52411 (DAPH) inhibits c-src kinase with an
IC
50
value of 16 μM. CGP52411 inhibits PKC isozymes isolated from porcine brain with an
IC
50
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]
.
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 IC 50 of 1 μM. c-src autophosphorylation was inhibited with an IC 50 of 16 μM. And also resulted in a concentration-dependent reduction in tyrosine phosphorylation of p 185c-erbB2 , with an estimated IC 50 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] .
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. |
Appearance
Solid
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
DMSO : 100 mg/mL ( 303.63 mM ; Need ultrasonic)
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 |
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):233
- [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.
Synonyms
