CGP 52411
CGP 52411 性质
| 熔点 | 199-202℃ |
|---|---|
| 密度 | 1.374 |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：~30 mg/mL |
| 酸度系数(pKa) | 9.06±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 橙色 |
CGP 52411 用途与合成方法
|
EGFR 0.3 μM (IC 50 ) |
Amyloid-β
|
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.
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).
Western Blot Analysis
| 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. |
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.
| 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 |
| Result: | Antitumor efficacy was obtained at doses between 50 mg/kg and 6.3 mg/kg. |
