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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。
CGP52411图片
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 p185c-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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM3.0363 mL15.1814 mL30.3628 mL
5 mM0.6073 mL3.0363 mL6.0726 mL
10 mM0.3036 mL1.5181 mL3.0363 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。