CGP52411
CAS No. 145915-58-8
CGP52411 ( DAPH )
产品货号. M26105 CAS No. 145915-58-8
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)。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥1320 | 有现货 |
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10MG | ¥2130 | 有现货 |
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25MG | ¥4277 | 有现货 |
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50MG | ¥6229 | 有现货 |
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100MG | ¥8748 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称CGP52411
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注意事项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
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产品简述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)。
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产品描述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.
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体外实验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.
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体内实验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.
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同义词DAPH
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通路Others
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靶点Other Targets
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受体Non-cleavable
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研究领域——
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适应症——
化学信息
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CAS Number145915-58-8
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分子量329.359
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分子式C20H15N3O2
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 100 mg/mL (303.63 mM)
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SMILESO=C1NC(=O)c2cc(Nc3ccccc3)c(Nc3ccccc3)cc12
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Pyrrolobenzodiazepine Dimer Antibody-Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers. J Med Chem. 2017 Dec 14;60(23):9490-9507.
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