CGP52411  ≥98%

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包装规格:5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介:一种高选择性,有效,口服活性和ATP竞争性的EGFR抑制剂,IC50为0.3μM。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。
溶解性:DMSO :100 mg/mL (303.63 mM;超声助溶)
储备液保存:-80°C, 6 months -20°C, 1 month
靶点:EGFR:0.3 μM (IC50);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 IC50s of 1 μM and 16 μM, respectively. CGP52411 treatment also shows a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2 with an IC50 value of 10 μM. CGP52411 (DAPH) inhibits c-src kinase with an IC50 value of 16 μM. CGP52411 inhibits PKC isozymes isolated from porcine brain with an IC50 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).
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.
保存条件:-20℃
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