1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Neuronal Signaling
  2. EGFR Amyloid-β
  3. CGP52411

CGP52411  (Synonyms: DAPH)

目录号: HY-103442 纯度: 99.71%
COA 产品使用指南

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。

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CGP52411 Chemical Structure

CGP52411 Chemical Structure

CAS No. : 145915-58-8

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10 mM * 1 mL in DMSO ¥841
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1 mg ¥528
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5 mg ¥1160
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10 mg ¥1740
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50 mg ¥4750
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease[1][2].

IC50 & Target[1][2]

EGFR

0.3 μM (IC50)

Amyloid-β

 

体外研究
(In Vitro)

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[1].
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)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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.
体内研究
(In Vivo)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice injected with A431cells[1]
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.
分子量

329.35

Formula

C20H15N3O2

CAS 号
性状

固体

颜色

Yellow to orange

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (303.63 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0363 mL 15.1814 mL 30.3628 mL
5 mM 0.6073 mL 3.0363 mL 6.0726 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.82%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0363 mL 15.1814 mL 30.3628 mL 75.9071 mL
5 mM 0.6073 mL 3.0363 mL 6.0726 mL 15.1814 mL
10 mM 0.3036 mL 1.5181 mL 3.0363 mL 7.5907 mL
15 mM 0.2024 mL 1.0121 mL 2.0242 mL 5.0605 mL
20 mM 0.1518 mL 0.7591 mL 1.5181 mL 3.7954 mL
25 mM 0.1215 mL 0.6073 mL 1.2145 mL 3.0363 mL
30 mM 0.1012 mL 0.5060 mL 1.0121 mL 2.5302 mL
40 mM 0.0759 mL 0.3795 mL 0.7591 mL 1.8977 mL
50 mM 0.0607 mL 0.3036 mL 0.6073 mL 1.5181 mL
60 mM 0.0506 mL 0.2530 mL 0.5060 mL 1.2651 mL
80 mM 0.0380 mL 0.1898 mL 0.3795 mL 0.9488 mL
100 mM 0.0304 mL 0.1518 mL 0.3036 mL 0.7591 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CGP52411
目录号:
HY-103442
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