CGP52411

立即咨询

CGP52411

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

145915-58-8

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议

产品名称

DAPH

产品介绍

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。

生物活性

CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitiveEGFRinhibitor with anIC₅₀of 0.3 μM. CGP52411 blocks the toxic influx of Ca²⁺ions into neuronal cells, and dramatic inhibits and reverses the formation ofβ-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 withIC₅₀s of 1 μM and 16 μM, respectively. CGP52411 treatment also shows a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2 with anIC₅₀value of 10 μM^[1].
CGP52411 (DAPH) inhibits c-src kinase with anIC₅₀value of 16 μM. CGP52411 inhibits PKC isozymes isolated from porcine brain with anIC₅₀of 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].

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 anIC₅₀of 1 μM. c-src autophosphorylation was inhibited with anIC₅₀of 16 μM. And also resulted in a concentration-dependent reduction in tyrosine phosphorylation of p^185c-erbB2, with an estimatedIC₅₀value 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].

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

性状

Solid

Formula

C₂₀H₁₅N₃O₂

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

溶解性数据

In Vitro:

DMSO : 100 mg/mL(303.63 mM;Need ultrasonic)

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
10 mM	0.3036 mL	1.5181 mL	3.0363 mL

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。