CGP 52411

生物活性靶点体外研究体内研究 CGP 52411 试剂级价格

CGP 52411

CAS号:145915-58-8
英文名:DAPH
中文名:CGP 52411
CBNumber:CB2498023
分子式:C20H15N3O2
分子量:329.35
MOL File:145915-58-8.mol

CGP 52411化学性质

熔点 :199-202℃
密度 :1.374
储存条件 :2-8°C
溶解度 :DMSO: ~30 mg/mL
酸度系数(pKa) :9.06±0.20(Predicted)
形态 :solid
颜色 :orange

安全信息

安全说明 :36/37
WGK Germany :3

CGP 52411性质、用途与生产工艺

生物活性 CGP52411 (DAPH) 是一种高选择性，有效，口服活性和 ATP 竞争性的 EGFR 抑制剂，IC50 为 0.3 μM。CGP52411 阻止有毒的 Ca2+ 离子流入神经元细胞，并显着抑制和逆转与阿尔茨海默症相关的 β-amyloid (Aβ42) 原纤维聚集物的形成。
靶点

EGFR

0.3 μM (IC ₅₀ )

Amyloid-β

体外研究

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.

体内研究

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.