Name | DAPH |
Synonyms | DAPH DAPH-1(DAPH 1H-Isoindole-1,3(2H)-dione, 5,6-bis(phenylamino)- 4,5-Dianilinophthalimide, 5,6-Bis(phenylamino)-1H-isoindole-1,3(2H)-dione, CGP 52411 |
CAS | 145915-58-8 |
EINECS | 406-050-3 |
Molecular Formula | C20H15N3O2 |
Molar Mass | 329.35 |
Density | 1.374 |
Melting Point | 199-202℃ |
Solubility | DMSO: ~30mg/mL |
Appearance | solid |
Color | orange |
pKa | 9.06±0.20(Predicted) |
Storage Condition | 2-8°C |
Physical and Chemical Properties | Solubility: DMSO: ~ 30 mg/mL storage condition: 2-8 ℃ WGK Germany:3 |
Safety Description | 36/37 - Wear suitable protective clothing and gloves. |
WGK Germany | 3 |
biological activity | CGP52411 (DAPH) is a highly selective, effective, oral activity and ATP competitive EGFR inhibitor with IC50 of 0.3 μM. CGP52411 blocked the influx of toxic Ca2 + ions into neuronal cells and significantly inhibited and reversed the formation of β-amyloid (Aβ42) fibrillar aggregates associated with Alzheimer's disease. |
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. Antitumor efficacy was obtained at doses between 50 mg/kg and 6.3 mg/kg. |
Animal Model: | Female BALB/c nude mice injected with A431cells |
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 |