CGP52411

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CGP52411 (DAPH) 是一种高选择性、口服活性、ATP 竞争性 EGFR 抑制剂 (IC50: 0.3 μM)。

CGP52411 (DAPH) is a highly selective, orally active, and ATP-competitive EGFR inhibitor (IC50: 0.3 μM). It blocks the toxic influx of Ca2+ ions into neuronal cells and dramatically inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates.(In Vitro):In A431 cells, CGP52411 (0-100 μM) dose-dependently inhibits autophosphorylation and c-src autophosphorylation with IC50s of 1 μM and 16 μM, respectively. CGP52411 reduces tyrosine phosphorylation of p185c-erbB2 in a concentration-dependent manner(IC50 = 10 μM).CGP52411 inhibits c-src kinase (IC50 = 16 μM) and PKC isozymes isolated from porcine brain (IC50 = 80 μM).(In Vivo):In female BALB/c nude mice, CGP52411 (6.3 mg/kg-50 mg/kg; orally) shows antitumor efficacy.

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). 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 IC50 of 1 μM. c-src autophosphorylation was inhibited with an IC50 of 16 μM. And also resulted in a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2, with an estimated IC50 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.

DAPH

Others

Other Targets

Non-cleavable

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145915-58-8

329.359

C20H15N3O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (303.63 mM)

O=C1NC(=O)c2cc(Nc3ccccc3)c(Nc3ccccc3)cc12

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(-20℃)

With Ice Pack

≥ 2 years