| 中文名称: | CGP52411 | ||||
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| 英文名称: | CGP52411 | ||||
| 别名: | CGP52411 DAPH | ||||
| CAS No: | 145915-58-8 | 分子式: | C20H15N3O2 | 分子量: | 329.35 |
| CAS No: | 145915-58-8 | ||||
| 分子式: | C20H15N3O2 | ||||
| 分子量: | 329.35 | ||||
| EINEC: | 406-050-3 | ||||
| EINEC: | 406-050-3 | ||||
基本信息
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产品编号：C11131 |
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产品名称：CGP52411 |
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CAS: |
145915-58-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
329.35 |
-20℃ |
一个月 |
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化学名： |
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生物活性
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产品描述 |
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。 |
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靶点/IC50 |
EGFR 0.3μM(IC50) |
Amyloid-β |
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体外研究 |
CGP52411 (DAPH;0-100μM; 90minutes; A431 cells) treatment inhibits autophosphorylation and c-src autophosphorylation in vitro in a dose-dependent manner with IC50s of 1μM and 16μM, respectively. CGP52411 treatment also shows a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2 with an IC50 value of 10μM . CGP52411 (DAPH) inhibits c-src kinase with an IC50 value of 16μM. CGP52411 inhibits PKC isozymes isolated from porcine brain with an IC50 of 80μM. 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 (aPKCη). |
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Cell Line: |
A431 cells |
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Concentration: |
0μM, 0.1μM, 1μM, 10μM, 50μM, 100μM |
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Incubation Time: |
90 minutes |
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Result: |
Inhibited autophosphorylation in vitro in a dose-dependent manner with an IC50 of 1μM. c-src autophosphorylation was inhibited with an IC50 of 16μM. And also resulted in a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2, with an estimated IC50 value of 10μM. |
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体内研究 |
CGP52411 (3.2mg/kg, 6.3mg/kg, 12.5mg/kg, 25mg/kg, and 50mg/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 activit
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Animal Model: |
Female BALB/c nude mice injected with A431cells. |
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Dosage: |
3.2mg/kg, 6.3mg/kg, 12.5mg/kg, 25mg/kg, and 50mg/kg. |
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Administration: |
Oral administration; daily; for 15 days. |
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Result: |
Antitumor efficacy was obtained at doses between 50mg/kg and 6.3mg/kg. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
