CGP52411 - CAS:145915-58-8

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CGP52411 (Synonyms:DAPH)

目录号 : KM10168 CAS No. : 145915-58-8 纯度 : 98%

Data Sheet 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。

规格	价格	是否有货	数量
5mg		In-stock

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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 Ca ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.

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).

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 p, with an estimated IC₅₀ value of 10 μM.

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.

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.

分子式

C₂₀H₁₅N₃O₂

分子量

329.35

CAS号

145915-58-8

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

纯度： 98%

Data Sheet

产品使用指南

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

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第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

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工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器